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Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.
J Med Chem 48: 4596-607 (2005)
Serono Pharmaceutical Research Institute
Identification of novel extracellular signal-regulated kinase docking domain inhibitors.
J Med Chem 48: 4586-95 (2005)
University of Maryland
Adamantyl cannabinoids: a novel class of cannabinergic ligands.
J Med Chem 48: 4576-85 (2005)
Northeastern University
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase.
J Med Chem 48: 4547-57 (2005)
Irbm (Merck Research Laboratories Rome)
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.
J Med Chem 48: 4535-46 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and biological evaluation of geminal disulfones as HIV-1 integrase inhibitors.
J Med Chem 48: 4526-34 (2005)
University of California
Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.
J Med Chem 48: 4511-25 (2005)
Aventis Pharma
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an"agreement docking" method.
J Med Chem 48: 4507-10 (2005)
Glaxosmithkline
Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.
Neuropsychopharmacology 31: 265-77 (2006)
Case Western Reserve University
Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.
Biochemistry 44: 9430-40 (2005)
Merck Research Laboratories
Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic alpha,beta-unsaturated esters.
Bioorg Med Chem 13: 5240-52 (2005)
National Taiwan University
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 15: 3834-7 (2005)
Zhejiang University
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
Bioorg Med Chem Lett 15: 3665-9 (2005)
Merck Sharp and Dohme Research Laboratories
Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.
Bioorg Med Chem Lett 15: 3925-9 (2005)
Merck
In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I.
Bioorg Med Chem Lett 15: 3930-3 (2005)
Università
A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series.
Bioorg Med Chem Lett 15: 3816-20 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.
Bioorg Med Chem Lett 15: 3744-7 (2005)
Harvard Medical School
Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.
Bioorg Med Chem Lett 15: 3891-5 (2005)
Glaxosmithkline
Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes.
Bioorg Med Chem Lett 15: 4100-4 (2005)
University of Mysore
Hydrophobicity in the design of P2/P2' tetrahydropyrimidinone HIV protease inhibitors.
Bioorg Med Chem Lett 15: 3767-70 (2005)
Clarkson University
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.
Bioorg Med Chem Lett 15: 3758-62 (2005)
University of Nottingham
2-Aminoquinazoline inhibitors of cyclin-dependent kinases.
Bioorg Med Chem Lett 15: 3881-5 (2005)
Naeja Pharmaceutical
QSAR of adenosine A3 receptor antagonist 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives using chemometric tools.
Bioorg Med Chem Lett 15: 3737-43 (2005)
Jadavpur University
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.
Bioorg Med Chem Lett 15: 3912-6 (2005)
Merck Research Laboratories
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Bioorg Med Chem Lett 15: 4143-50 (2005)
Seoul National University
Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.
Bioorg Med Chem Lett 15: 3778-81 (2005)
Glaxosmithkline
L-arginine analogs as alternate substrates for nitric oxide synthase.
Bioorg Med Chem Lett 15: 3934-41 (2005)
University of California
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives.
Bioorg Med Chem Lett 15: 3732-6 (2005)
Graduate School of The Chinese Academy of Sciences
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.
Bioorg Med Chem Lett 15: 3900-7 (2005)
Bayer Healthcare
BCUT descriptors to predicting affinity toward A3 adenosine receptors.
Bioorg Med Chem Lett 15: 3491-5 (2005)
Experimental Sugar Cane Station&Quot;Villa Clara-Cienfuegos&Quot
The molecular basis for coxib inhibition of p38alpha MAP kinase.
Bioorg Med Chem Lett 15: 3506-9 (2005)
Universidade Federal Do Rio De Janeiro (Ufrj)
Interaction of chiral MS-245 analogs at h5-HT6 receptors.
Bioorg Med Chem Lett 15: 3510-3 (2005)
Virginia Commonwealth University
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.
Bioorg Med Chem Lett 15: 3519-23 (2005)
Glaxosmithkline
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.
Bioorg Med Chem Lett 15: 3870-3 (2005)
Pharmaceutical Research Institute
Synthesis of an N-acyl sulfamate analog of luciferyl-AMP: a stable and potent inhibitor of firefly luciferase.
Bioorg Med Chem Lett 15: 3860-4 (2005)
Connecticut College
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.
J Biol Chem 280: 31220-9 (2005)
Chinese Academy of Sciences
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by alpha-aminoxy acids.
Bioorg Med Chem Lett 15: 2986-2989 (2005)
TBA
Efficient synthetic inhibitors of anthrax lethal factor.
Proc Natl Acad Sci U S A 102: 9499-504 (2005)
Burnham Institute For Medical Research
Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists.
Bioorg Med Chem Lett 15: 4029-32 (2005)
Pharmaceutical Research Institute
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 15: 3540-6 (2005)
Glaxosmithkline
3-Thio-1,2,4-triazoles, novel somatostatin sst2/sst5 agonists.
Bioorg Med Chem Lett 15: 3555-9 (2005)
Institut Henri Beaufour
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
Bioorg Med Chem Lett 15: 3568-72 (2005)
University of Virginia
Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1.
Bioorg Med Chem Lett 15: 3514-8 (2005)
Wyeth Research
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Bioorg Med Chem Lett 15: 3501-5 (2005)
Merck Research Laboratories
Investigation of glycine alpha-ketoamide HCV NS3 protease inhibitors: effect of carboxylic acid isosteres.
Bioorg Med Chem Lett 15: 3487-90 (2005)
Pharmaceutical Research Institute
Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.
Bioorg Med Chem Lett 15: 3696-700 (2005)
Pharmacopeia Drug Discovery
SAR studies of 6-aryl-1,3-dihydrobenzimidazol-2-ones as progesterone receptor antagonists.
Bioorg Med Chem Lett 15: 3600-3 (2005)
Wyeth Research
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1.
Bioorg Med Chem Lett 15: 3670-4 (2005)
Schering-Plough Research Institute
Dibenzodioxocinones--a new class of CETP inhibitors.
Bioorg Med Chem Lett 15: 3611-4 (2005)
Bayer Healthcare Pharma Research
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.
Bioorg Med Chem Lett 15: 3560-4 (2005)
Glaxosmithkline
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.
Bioorg Med Chem Lett 15: 3604-8 (2005)
Vernalis Research
Features of selective kinase inhibitors.
Chem Biol 12: 621-37 (2005)
University of California San Francisco
Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.
J Nat Prod 68: 947-50 (2005)
University of Mississippi
Constituents of the leaves of Macaranga tanarius.
J Nat Prod 68: 927-30 (2005)
Ramkhamhaeng University
Indole alkaloids and other constituents of Rauwolfia serpentina.
J Nat Prod 68: 848-52 (2005)
Kobe Pharmaceutical University
Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.
J Med Chem 48: 4469-73 (2005)
National Taiwan University
Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
J Med Chem 48: 4457-68 (2005)
Merck Research Laboratories
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
J Med Chem 48: 4444-56 (2005)
University of Bologna
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.
J Med Chem 48: 4420-31 (2005)
Harvard Medical School
Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
J Med Chem 48: 4410-9 (2005)
Martin-Luther-University Halle-Wittenberg
Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II.
J Med Chem 48: 4400-9 (2005)
LinköPing University
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
J Med Chem 48: 4378-88 (2005)
Sapienza University of Rome
Quinic acid derivatives as sialyl Lewis(x)-mimicking selectin inhibitors: design, synthesis, and crystal structure in complex with E-selectin.
J Med Chem 48: 4346-57 (2005)
Wyeth
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.
J Med Chem 48: 4332-45 (2005)
Vernalis (R&D)
2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
J Med Chem 48: 4312-31 (2005)
Domp£
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.
J Med Chem 48: 4254-65 (2005)
Emory University
Functionalized pyrrolidines inhibit alpha-mannosidase activity and growth of human glioblastoma and melanoma cells.
J Med Chem 48: 4237-46 (2005)
Institute of Chemical Sciences and Engineering
Peptoid-peptide hybrids as potent novel melanocortin receptor ligands.
J Med Chem 48: 4224-30 (2005)
Utrecht University
Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors.
J Med Chem 48: 4220-3 (2005)
Sapienza University of Rome
A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists.
J Med Chem 48: 4216-9 (2005)
Universidad Complutense
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
J Med Chem 48: 4212-5 (2005)
Vernalis (R&D)
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.
J Med Chem 48: 4208-11 (2005)
Johnson & Johnson Pharmaceutical
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists.
J Med Chem 48: 4204-7 (2005)
Università
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
J Med Chem 48: 4200-3 (2005)
Eli Lilly
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.
J Enzyme Inhib Med Chem 20: 135-41 (2005)
Cardiff University
3-(1,2,3-Triazol-1-yl)-1-thio-galactosides as small, efficient, and hydrolytically stable inhibitors of galectin-3.
Bioorg Med Chem Lett 15: 3344-6 (2005)
Lund University
Rhodanine derivatives as inhibitors of JSP-1.
Bioorg Med Chem Lett 15: 3374-9 (2005)
Ceptyr
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.
Cancer Res 65: 5399-407 (2005)
Cyclacel
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
Bioorg Med Chem Lett 15: 3407-11 (2005)
Glaxosmithkline
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
Bioorg Med Chem Lett 15: 3338-43 (2005)
The Institute of Cancer Research
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.
Bioorg Med Chem 13: 4835-41 (2005)
Hoffmann-La Roche
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis.
Bioorg Med Chem Lett 15: 3691-5 (2005)
Pharmacopeia Drug Discovery
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.
Bioorg Med Chem Lett 15: 3352-5 (2005)
Merck Frosst Centre For Therapeutic Research
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Bioorg Med Chem Lett 15: 3385-8 (2005)
Pfizer
Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.
Biochemistry 44: 8643-51 (2005)
Case Western Reserve University
Differential effects of the 5-hydroxytryptamine (5-HT)1A receptor inverse agonists Rec 27/0224 and Rec 27/0074 on electrophysiological responses to 5-HT1A receptor activation in rat dorsal raphe nucleus and hippocampus in vitro.
J Pharmacol Exp Ther 315: 109-17 (2005)
Universit&Aagrove
Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties.
J Pharmacol Exp Ther 314: 1274-89 (2005)
Wyeth
Deoxyribosyl analogues of methionyl and isoleucyl sulfamate adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.
Bioorg Med Chem Lett 15: 3389-93 (2005)
Seoul National University
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bioorg Med Chem Lett 15: 3430-3 (2005)
Merck Research Laboratories
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.
Bioorg Med Chem Lett 15: 3685-90 (2005)
Neurocrine Biosciences
Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor.
Bioorg Med Chem Lett 15: 3446-9 (2005)
F. Hoffmann-La Roche
Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity.
Bioorg Med Chem Lett 15: 3459-62 (2005)
Astrazeneca
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 15: 3434-8 (2005)
Neurocrine Biosciences
Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Bioorg Med Chem Lett 15: 3439-45 (2005)
Neurocrine Biosciences
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
Bioorg Med Chem Lett 15: 3402-6 (2005)
Glaxosmithkline
(2R)-2-methylchromane-2-carboxylic acids: discovery of selective PPARalpha agonists as hypolipidemic agents.
Bioorg Med Chem Lett 15: 3347-51 (2005)
Merck Research Laboratories
Identification of aminopiperidine benzamides as MCHr1 antagonists.
Bioorg Med Chem Lett 15: 3412-6 (2005)
Abbott Laboratories
Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease.
Biochem Biophys Res Commun 333: 194-9 (2005)
National Taiwan University
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
J Pharmacol Exp Ther 314: 1310-21 (2005)
Vrije Universiteit Amsterdam
Carboxylate bioisosteres of gabapentin.
Bioorg Med Chem Lett 16: 2333-6 (2006)
Pfizer
Rapid computational identification of the targets of protein kinase inhibitors.
J Med Chem 48: 4138-52 (2005)
University of Iowa
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.
J Med Chem 48: 4100-10 (2005)
Neurocrine Biosciences
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
J Med Chem 48: 4087-99 (2005)
Arizona State University
Novel nonsteroidal antiinflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies.
J Med Chem 48: 4061-7 (2005)
University of Alberta
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.
J Med Chem 48: 4049-60 (2005)
University of Parma
Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4. An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
J Med Chem 48: 4025-30 (2005)
University of Pennsylvania
New selective AT2 receptor ligands encompassing a gamma-turn mimetic replacing the amino acid residues 4-5 of angiotensin II act as agonists.
J Med Chem 48: 4009-24 (2005)
Uppsala University
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
J Med Chem 48: 3991-4008 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
J Med Chem 48: 3980-90 (2005)
Abbott Laboratories
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
J Med Chem 48: 3953-79 (2005)
Wyeth Research
Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform.
J Med Chem 48: 3945-8 (2005)
National Cancer Institute-Frederick
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia.
Bioorg Med Chem Lett 15: 3197-200 (2005)
Merck Research Laboratories
Sialyl Lewis(x) analogs based on a quinic acid scaffold as the fucose mimic.
Bioorg Med Chem Lett 15: 3224-8 (2005)
National Chemical Engineering Institute In Paris
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.
Bioorg Med Chem Lett 15: 3229-32 (2005)
Glaxosmithkline
A three-residue, continuous binding epitope peptidomimetic of ShK toxin as a Kv1.3 inhibitor.
Bioorg Med Chem Lett 15: 3193-6 (2005)
Institute of Medical Research
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.
Bioorg Med Chem Lett 15: 3279-83 (2005)
Fujisawa Pharmaceutical
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
Bioorg Med Chem Lett 15: 3284-7 (2005)
Fujisawa Pharmaceutical
In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants.
NA
Oregon Health and Science University Cancer Institute
Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist.
Bioorg Med Chem Lett 15: 3292-5 (2005)
Roche Palo Alto
Ethers of 3-hydroxyphenylacetic acid as selective gamma-hydroxybutyric acid receptor ligands.
Bioorg Med Chem Lett 15: 3201-2 (2005)
University of Maryland
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
Bioorg Med Chem Lett 15: 3271-5 (2005)
National Health Research Institutes
6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.
Bioorg Med Chem Lett 15: 3237-40 (2005)
Virginia Commonwealth University
Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.
Bioorg Med Chem Lett 15: 3241-6 (2005)
Semmelweis University
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
Bioorg Med Chem Lett 15: 3203-6 (2005)
Glaxosmithkline
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.
Bioorg Med Chem Lett 15: 3257-62 (2005)
Peking University
Novel phomactin analogues as PAF receptor ligands.
Bioorg Med Chem Lett 15: 3263-6 (2005)
The University of Nottingham
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents.
Bioorg Med Chem Lett 15: 3296-301 (2005)
Merck Research Laboratories
Petrosamine B, an inhibitor of the Helicobacter pylori enzyme aspartyl semialdehyde dehydrogenase from the Australian sponge Oceanapia sp.
J Nat Prod 68: 804-6 (2005)
Griffith University
Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound.
J Nat Prod 68: 674-7 (2005)
University of Antwerp
Structural bioinformatics-based design of selective, irreversible kinase inhibitors.
Science 308: 1318-21 (2005)
University of California
3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: synthesis and biological evaluation.
J Med Chem 48: 3930-4 (2005)
Nitromed
Inhibition of herpes simplex virus thymidine kinases by 2-phenylamino-6-oxopurines and related compounds: structure-activity relationships and antiherpetic activity in vivo.
J Med Chem 48: 3919-29 (2005)
Glsynthesis
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles.
J Med Chem 48: 3891-902 (2005)
Wyeth Research
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
J Med Chem 48: 3858-73 (2005)
University of Genoa
Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.
J Med Chem 48: 3852-7 (2005)
Research Triangle Institute
Design, synthesis and antiviral activity of novel 4,5-disubstituted 7-(beta-D-ribofuranosyl)pyrrolo[2,3-d][1,2,3]triazines and the novel 3-amino-5-methyl-1-(beta-D-ribofuranosyl)- and 3-amino-5-methyl-1-(2-deoxy-beta-D-ribofuranosyl)-1,5-dihydro-1,4,5,6,7,8-hexaazaacenaphthylene as analogues of tri
J Med Chem 48: 3840-51 (2005)
University of Michigan
Design of small-sized libraries by combinatorial assembly of linkers and functional groups to a given scaffold: application to the structure-based optimization of a phosphodiesterase 4 inhibitor.
J Med Chem 48: 3816-22 (2005)
Umr Cnrs 7081
Predictive three-dimensional quantitative structure-activity relationship of cytochrome P450 1A2 inhibitors.
J Med Chem 48: 3808-15 (2005)
University of Kuopio
Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.
J Med Chem 48: 3776-83 (2005)
Cephalon
Comparison of ligand-based and structure-based 3D-QSAR approaches: a case study on (aryl-)bridged 2-aminobenzonitriles inhibiting HIV-1 reverse transcriptase.
J Med Chem 48: 3756-67 (2005)
University of Perugia
Decoys for docking.
J Med Chem 48: 3714-28 (2005)
University of California San Francisco
Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
J Med Chem 48: 3704-13 (2005)
University of Washington At Seattle
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
J Med Chem 48: 3696-9 (2005)
Friedrich-Alexander University
Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors.
J Med Chem 48: 3680-3 (2005)
Chemical Diversity Research Institute
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
J Med Chem 48: 3663-79 (2005)
National Institute On Drug Abuse-Intramural Research Program
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
Bioorg Med Chem Lett 15: 3091-5 (2005)
Fujisawa Pharmaceutical
Synthetic lanostane-type triterpenoids as inhibitors of DNA topoisomerase II.
Bioorg Med Chem Lett 15: 2966-9 (2005)
Osaka University of Pharmaceutical Sciences
New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects.
Bioorg Med Chem Lett 15: 2990-3 (2005)
Daiichi Suntory Biomedical Research
4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors.
Bioorg Med Chem Lett 15: 2998-3001 (2005)
Korea Research Institute of Chemical Technology
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa.
Bioorg Med Chem Lett 15: 3006-11 (2005)
Pfizer
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
Bioorg Med Chem 13: 4063-70 (2005)
Ohio State University
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.
Bioorg Med Chem Lett 15: 2926-31 (2005)
Merck Research Laboratories
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.
Bioorg Med Chem Lett 15: 2918-22 (2005)
Abbott Laboratories
Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.
Bioorg Med Chem Lett 15: 2910-3 (2005)
Vrije Universiteit Amsterdam
New inhibitors of rabbit muscle triose-phosphate isomerase.
Bioorg Med Chem Lett 15: 2906-9 (2005)
Paris-Sud University
Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism.
Bioorg Med Chem Lett 15: 2898-901 (2005)
Janssen-Cilag
Synthesis, in vivo and in vitro biological activity of novel azaline B analogs.
Bioorg Med Chem Lett 15: 2894-7 (2005)
Salk Institute
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.
Bioorg Med Chem Lett 15: 2891-3 (2005)
Chinese Academy of Sciences
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
Bioorg Med Chem Lett 15: 2886-90 (2005)
Reverse Proteomics Research Institute
Evaluation of 3-substituted arginine analogs as selective inhibitors of human nitric oxide synthase isozymes.
Bioorg Med Chem Lett 15: 2881-5 (2005)
Nagoya City University
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.
Bioorg Med Chem Lett 15: 2870-5 (2005)
Pfizer
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Bioorg Med Chem Lett 15: 2865-9 (2005)
Wyeth Research
Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors.
Bioorg Med Chem Lett 15: 2857-60 (2005)
Institute of Science & Technology
Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization.
Bioorg Med Chem Lett 15: 2840-4 (2005)
The Scripps Research Institute
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
Bioorg Med Chem Lett 15: 2824-8 (2005)
Merck Research Laboratories
Design, synthesis, and evaluation of proline based melanocortin receptor ligands.
Bioorg Med Chem Lett 15: 2819-23 (2005)
Procter & Gamble Pharmaceuticals
Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid.
Bioorg Med Chem Lett 15: 2812-8 (2005)
Pfizer
Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13.
Bioorg Med Chem Lett 15: 2808-11 (2005)
Pfizer
Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as adenosine kinase inhibitors.
Bioorg Med Chem Lett 15: 2803-7 (2005)
Abbott Laboratories
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.
Bioorg Med Chem Lett 15: 2771-5 (2005)
Merck Research Laboratories
Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors.
Bioorg Med Chem Lett 15: 2758-60 (2005)
University of Tennessee
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Bioorg Med Chem Lett 15: 2752-7 (2005)
Abbott Laboratories
Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.
Bioorg Med Chem Lett 15: 2734-7 (2005)
Aventis Pharmaceuticals
Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.
Bioorg Med Chem Lett 15: 2970-3 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Bioorg Med Chem Lett 15: 2974-9 (2005)
Pfizer
The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: antagonists versus agonists.
Bioorg Med Chem Lett 15: 3020-3 (2005)
Schering-Plough Research Institute
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 15: 3048-52 (2005)
Merck Research Laboratories
Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes.
Bioorg Med Chem Lett 15: 3096-101 (2005)
Ospedale San Lazzaro
QSAR analysis of thiazole benzenesulfonamide substituted 3-pyridylethanolamines as beta3-adrenergic receptor agonist.
Bioorg Med Chem Lett 15: 3167-73 (2005)
S.G.S.I.T.S.
Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumors.
Bioorg Med Chem Lett 15: 3302-6 (2005)
Università
Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.
Bioorg Med Chem Lett 15: 3102-8 (2005)
Universita Degli Studi Di Firenze
Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin.
J Pharmacol Exp Ther 314: 876-82 (2005)
University of Tokyo
NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors.
J Biol Chem 280: 30273-81 (2005)
India Central Drug Research Institute
Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.
Bioorg Med Chem Lett 15: 3058-62 (2005)
Development Center For Biotechnology
Acyclic cyanamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 15: 3039-43 (2005)
Glaxosmithkline
Structure-activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors.
Bioorg Med Chem Lett 15: 3109-13 (2005)
Tohoku University
Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase.
J Enzyme Inhib Med Chem 20: 61-7 (2005)
Crefsip
Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones.
J Enzyme Inhib Med Chem 20: 41-7 (2005)
Quaid-I-Azam University
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease.
Bioorg Med Chem Lett 15: 3086-90 (2005)
University of Debrecen
Hologram quantitative structure-activity relationships for a series of farnesoid X receptor activators.
Bioorg Med Chem Lett 15: 3119-25 (2005)
Universidade De SãO Paulo
4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 2. SAR.
Bioorg Med Chem Lett 15: 3053-7 (2005)
Bayer Research Center
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
J Med Chem 48: 3654-8 (2005)
Universidad Central De Venezuela
Are L-adenosine and its derivatives substrates for S-adenosyl-L-homocysteine hydrolase?
J Med Chem 48: 3649-53 (2005)
Florida International University
A new structural motif for mu-opioid antagonists.
J Med Chem 48: 3644-8 (2005)
Vrije Universiteit Brussel
Optimization of amide-based inhibitors of soluble epoxide hydrolase with improved water solubility.
J Med Chem 48: 3621-9 (2005)
Department of Entomology and University of California Davis Cancer Center
Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1.
J Med Chem 48: 3613-20 (2005)
Vanderbilt University
Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
J Med Chem 48: 3605-12 (2005)
Eli Lilly
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.
J Med Chem 48: 3586-604 (2005)
Central Pharmaceutical Research Institute
Structure-based design: synthesis and biological evaluation of a series of novel cycloamide-derived HIV-1 protease inhibitors.
J Med Chem 48: 3576-85 (2005)
University of Illinois At Chicago
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties.
J Med Chem 48: 3564-75 (2005)
University of Siena
AFMoC enhances predictivity of 3D QSAR: a case study with DOXP-reductoisomerase.
J Med Chem 48: 3547-63 (2005)
Philipps University
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
J Med Chem 48: 3478-80 (2005)
Glaxosmithkline
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.
J Med Chem 48: 3474-7 (2005)
Pfizer
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.
J Med Chem 48: 3467-70 (2005)
Wyeth Research
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.
J Med Chem 48: 3463-6 (2005)
University of Southern California
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
J Med Chem 48: 3449-62 (2005)
Monash University (Parkville Campus)
Pyrazole derivatives as photosynthetic electron transport inhibitors: new leads and structure-activity relationship.
J Agric Food Chem 53: 3848-55 (2005)
University of Ferrara
Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue.
J Pharmacol Exp Ther 314: 575-83 (2005)
Duquesne University
Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma.
J Pharmacol Exp Ther 314: 568-74 (2005)
Imperial College
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.
Bioorg Med Chem Lett 15: 2790-4 (2005)
Chinese Academy of Sciences
Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 15: 2711-5 (2005)
Universidad Nacional De Rosario
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Bioorg Med Chem Lett 15: 2943-7 (2005)
Merck Research Laboratories
Total asymmetric synthesis of (-)-conduramine B-1 and of its enantiomer. N-Benzyl derivatives of conduramine B-1 are beta-glucosidase inhibitors.
Bioorg Med Chem Lett 15: 3071-5 (2005)
Ecole Polytechnique FéDéRale De Lausanne (Epfl)
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.
Bioorg Med Chem Lett 15: 3137-42 (2005)
Wyeth Research
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.
Bioorg Med Chem Lett 15: 3081-5 (2005)
Novartis Institutes For Biomedical Research
The dietary polyphenol ellagic acid is a potent inhibitor of hOAT1.
Drug Metab Dispos 33: 1097-100 (2005)
Medical University of South Carolina
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
Bioorg Med Chem Lett 15: 2761-5 (2005)
Mclean Hospital
First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.
Biochemistry 44: 6858-66 (2005)
University of Bath
Aryl sulfones: a new class of gamma-secretase inhibitors.
Bioorg Med Chem Lett 15: 2685-8 (2005)
Merck Sharp & Dohme Research Laboratories
Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids.
Bioorg Med Chem Lett 15: 2679-84 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Identification of chemokine receptor CCR4 antagonist.
Bioorg Med Chem Lett 15: 2669-72 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of novel diphenacoum-derived, conformation-restricted vitamin K 2,3-epoxide reductase inhibitors.
Bioorg Med Chem Lett 15: 2665-8 (2005)
Tunghai University
Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.
Bioorg Med Chem Lett 15: 2647-52 (2005)
Adolor
Geometry, topology, and atom-weights assembly descriptors to predicting A1 adenosine receptors agonists.
Bioorg Med Chem Lett 15: 2641-5 (2005)
Experimental Sugar Cane Station
5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues.
Bioorg Med Chem Lett 15: 2611-5 (2005)
Pfizer
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Bioorg Med Chem Lett 15: 2565-9 (2005)
Taisho Pharmaceutical
A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.
Bioorg Med Chem Lett 15: 2541-6 (2005)
Neurocrine Biosciences
Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones.
Bioorg Med Chem Lett 15: 2537-40 (2005)
Nps Pharmaceuticals
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 15: 2533-6 (2005)
Merck Research Laboratories
4-Alkyl and 4,4'-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives as new inhibitors of bacterial cell wall biosynthesis.
Bioorg Med Chem Lett 15: 2527-31 (2005)
Wyeth Research
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.
Bioorg Med Chem Lett 15: 2523-6 (2005)
Roche Palo Alto
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.
Bioorg Med Chem Lett 15: 2519-22 (2005)
Neurocrine Biosciences
Structure-based design of protein tyrosine phosphatase-1B inhibitors.
Bioorg Med Chem Lett 15: 2503-7 (2005)
Astrazeneca
Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid.
Bioorg Med Chem Lett 15: 2481-6 (2005)
Pfizer
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.
Bioorg Med Chem Lett 15: 2471-5 (2005)
University of Arizona
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
Bioorg Med Chem Lett 15: 2467-9 (2005)
University of Catania
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Bioorg Med Chem Lett 15: 2461-5 (2005)
Acenta Discovery
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.
Bioorg Med Chem Lett 15: 2441-5 (2005)
Mitsubishi Pharma
Selective PPARgamma modulators with improved pharmacological profiles.
Bioorg Med Chem Lett 15: 2437-40 (2005)
Merck Research Laboratories
Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.
J Med Chem 48: 3438-42 (2005)
The Danish University of Pharmaceutical Sciences
Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.
J Med Chem 48: 3433-7 (2005)
Universita Di Messina
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.
J Med Chem 48: 3428-32 (2005)
Sapienza University of Rome
C-5-disubstituted barbiturates as potential molecular probes for noninvasive matrix metalloproteinase imaging.
J Med Chem 48: 3400-9 (2005)
University Hospital of The Westf£Lische Wilhelms-Universit£T
Adenosine kinase inhibitors. 4. 6,8-Disubstituted purine nucleoside derivatives. Synthesis, conformation, and enzyme inhibition.
J Med Chem 48: 3389-99 (2005)
Metabasis Therapeutics
Design of benzophenone-containing photoactivatable linear vasopressin antagonists: pharmacological and photoreactive properties.
J Med Chem 48: 3379-88 (2005)
University of Montpellier
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.
J Med Chem 48: 3372-8 (2005)
Sapienza University of Rome
Symmetrical bis-quinolinium compounds: new human choline kinase inhibitors with antiproliferative activity against the HT-29 cell line.
J Med Chem 48: 3354-63 (2005)
Universidad De Granada
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
J Med Chem 48: 3344-53 (2005)
Sapienza University of Rome
Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter.
J Med Chem 48: 3337-43 (2005)
University of Ferrara
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
J Med Chem 48: 3328-36 (2005)
University of Florida
Structure-activity relationships of fluorinated lysophosphatidic acid analogues.
J Med Chem 48: 3319-27 (2005)
The University of Utah
Conformation mining: an algorithm for finding biologically relevant conformations.
J Med Chem 48: 3313-8 (2005)
Rational Discovery
Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.
J Med Chem 48: 3290-312 (2005)
Aventis Pharma Deutschland
Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide scaffolds.
J Med Chem 48: 3280-9 (2005)
Kyoto University
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.
J Med Chem 48: 3239-50 (2005)
University of Szeged
Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening.
J Med Chem 48: 3221-30 (2005)
Protana
Successful in silico discovery of novel nonsteroidal ligands for human sex hormone binding globulin.
J Med Chem 48: 3203-13 (2005)
University of British Columbia
Synthesis and antibacterial activity of 1-(2-fluorovinyl)-7-substituted-4-quinolone-3-carboxylic acid derivatives, conformationally restricted analogues of fleroxacin.
J Med Chem 48: 3194-202 (2005)
Kyorin Pharmaceutical
Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands.
J Med Chem 48: 3171-81 (2005)
University of Michigan
Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor.
J Med Chem 48: 3153-63 (2005)
Università
Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.
J Med Chem 48: 3141-52 (2005)
The Institute For Diabetes Discovery
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities.
J Med Chem 48: 3118-21 (2005)
Abbott Laboratories
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.
J Med Chem 48: 3114-7 (2005)
Karo Bio
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities.
J Med Chem 48: 3110-3 (2005)
University of Ljubljana
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.
J Med Chem 48: 3107-9 (2005)
Gsk
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
J Med Chem 48: 3103-6 (2005)
Fujisawa Pharmaceutical
Discovery of a beta-MSH-derived MC-4R selective agonist.
J Med Chem 48: 3095-8 (2005)
Eli Lilly
Pharmacodynamic characterization of ZP120 (Ac-RYYRWKKKKKKK-NH2), a novel, functionally selective nociceptin/orphanin FQ peptide receptor partial agonist with sodium-potassium-sparing aquaretic activity.
J Pharmacol Exp Ther 314: 652-60 (2005)
Louisiana State University
Chemistry and biology of dihydroisoxazole derivatives: selective inhibitors of human transglutaminase 2.
Chem Biol 12: 469-75 (2005)
Stanford University
Switching between allosteric and dimerization inhibition of HIV-1 protease.
Chem Biol 12: 439-44 (2005)
Purdue University
Novel behavior of O-methylated beta-cyclodextrins in inclusion of meso-tetraarylporphyrins.
J Org Chem 70: 3667-73 (2005)
Doshisha University
Structures and aldose reductase inhibitory effects of bromophenols from the red alga Symphyocladia latiuscula.
J Nat Prod 68: 620-2 (2005)
Jilin Province Academy of Traditional Chinese Medicine and Materia Medica
Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.
J Nat Prod 68: 617-9 (2005)
Merck Research Laboratories
Tenellones A and B from a Diaporthe sp.: two highly substituted benzophenone inhibitors of parasite cGMP-dependent protein kinase activity.
J Nat Prod 68: 611-3 (2005)
Merck Research Laboratories
The psammaplysenes, specific inhibitors of FOXO1a nuclear export.
J Nat Prod 68: 574-6 (2005)
Harvard Medical School
Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.
J Nat Prod 68: 572-3 (2005)
Mitsubishi Pharma
QSAR for phospholipase A2 inhibitions by 1-acyloxy-3-N-n-octylcarbamyl-benzenes.
Bioorg Med Chem Lett 15: 2405-8 (2005)
National Chung-Hsing University
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
Bioorg Med Chem Lett 15: 2399-403 (2005)
Procter and Gamble Pharmaceuticals
2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.
Bioorg Med Chem Lett 15: 2385-8 (2005)
Merck Research Laboratories
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
Bioorg Med Chem Lett 15: 2381-4 (2005)
RhôNe-Poulenc Rorer
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.
Bioorg Med Chem Lett 15: 2371-4 (2005)
Pfizer
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Bioorg Med Chem Lett 15: 2365-9 (2005)
Schering-Plough Research Institute
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds.
Bioorg Med Chem Lett 15: 2359-64 (2005)
Ospedale San Lazzaro
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides--a new zinc-binding function in the design of inhibitors.
Bioorg Med Chem Lett 15: 2353-8 (2005)
Universita Degli Studi Di Firenze
Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols.
Bioorg Med Chem Lett 15: 2347-52 (2005)
University of Bucharest
Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies.
Bioorg Med Chem Lett 15: 2315-20 (2005)
University of Naples Federico Ii
A new development of matrix metalloproteinase inhibitors: twin hydroxamic acids as potent inhibitors of MMPs.
Bioorg Med Chem Lett 15: 2311-4 (2005)
Università
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase.
Bioorg Med Chem Lett 15: 2305-9 (2005)
Gsk
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor.
Bioorg Med Chem Lett 15: 2295-9 (2005)
Celltech R&D
Oximinoarylsulfonamides as potent HIV protease inhibitors.
Bioorg Med Chem Lett 15: 2275-8 (2005)
Abbott Laboratories
Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives.
Bioorg Med Chem Lett 15: 2265-9 (2005)
Kyoto 619-0216
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor.
Bioorg Med Chem Lett 15: 2259-63 (2005)
Merck Research Laboratories
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.
Bioorg Med Chem Lett 15: 2253-8 (2005)
Merck Research Laboratories
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.
Bioorg Med Chem Lett 15: 2249-52 (2005)
Berlex Biosciences
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Bioorg Med Chem Lett 15: 2235-8 (2005)
Kudos Horsham
NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives.
Bioorg Med Chem Lett 15: 2231-4 (2005)
Ludwig-Maximilians-UniversitäT MüNchen
Novel 2-amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase.
Bioorg Med Chem Lett 15: 2225-30 (2005)
Duquesne University
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.
Bioorg Med Chem Lett 15: 2221-4 (2005)
Johnson & Johnson Pharmaceutical
Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action.
Bioorg Med Chem Lett 15: 2215-9 (2005)
Dartmouth College
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 15: 2209-13 (2005)
Glaxosmithkline
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.
Bioorg Med Chem Lett 15: 2203-7 (2005)
Glaxosmithkline
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.
J Pharmacol Exp Ther 314: 77-85 (2005)
Taisho Pharmaceutical
Synthesis and anticancer activity of new pyrrolocarbazoles and pyrrolo-beta-carbolines.
Bioorg Med Chem 13: 2263-83 (2005)
Cnrs
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.
J Med Chem 48: 3080-4 (2005)
Nerviano Medical Sciences
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
J Med Chem 48: 3076-9 (2005)
Lundbeck Research Usa
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
J Med Chem 48: 3060-75 (2005)
University of Florida
Applying linear interaction energy method for rational design of noncompetitive allosteric inhibitors of the sarco- and endoplasmic reticulum calcium-ATPase.
J Med Chem 48: 3005-14 (2005)
Johns Hopkins University
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
J Med Chem 48: 2972-84 (2005)
University of Maryland
Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.
J Med Chem 48: 2964-71 (2005)
Glaxosmithkline
Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.
J Med Chem 48: 2957-63 (2005)
University of Illinois At Urbana-Champaign
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.
J Med Chem 48: 2944-56 (2005)
Nerviano Medical Sciences
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
J Med Chem 48: 2936-43 (2005)
Università
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.
J Med Chem 48: 2906-15 (2005)
University of Mississippi
Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.
J Med Chem 48: 2892-905 (2005)
Memorial Sloan-Kettering Cancer Center
(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
J Med Chem 48: 2882-91 (2005)
Korea Research Institute of Chemical Technology
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol.
J Med Chem 48: 2876-81 (2005)
Medical University of South Carolina
Design, synthesis, and antiviral activity of adenosine 5'-phosphonate analogues as chain terminators against hepatitis C virus.
J Med Chem 48: 2867-75 (2005)
Valeant Pharmaceuticals International
N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo.
J Med Chem 48: 2778-89 (2005)
Technische Universit£T M£Nchen
Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors.
J Med Chem 48: 2759-62 (2005)
University of Bath
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction.
J Am Chem Soc 127: 5463-8 (2005)
Yale University
Synthesis and evaluation of potential inhibitors of eIF4E cap binding to 7-methyl GTP.
Bioorg Med Chem Lett 15: 2177-80 (2005)
University of Minnesota
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Bioorg Med Chem Lett 15: 2163-7 (2005)
Merck Research Laboratories
The role of QSAR in dopamine interactions.
Bioorg Med Chem Lett 15: 2149-57 (2005)
Pomona College
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Bioorg Med Chem Lett 15: 2129-34 (2005)
Merck Research Laboratories
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
Bioorg Med Chem Lett 15: 2119-22 (2005)
Schering-Plough Research Institute
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
Bioorg Med Chem Lett 15: 2107-10 (2005)
Rensselaer Polytechnic Institute
Discovery, synthesis and biological evaluation of novel glucokinase activators.
Bioorg Med Chem Lett 15: 2103-6 (2005)
Astrazeneca
QSAR analyses of conformationally restricted 1,5-diaryl pyrazoles as selective COX-2 inhibitors: application of connection table representation of ligands.
Bioorg Med Chem Lett 15: 2097-102 (2005)
Devi Ahilya Vishwavidyalaya
Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.
Bioorg Med Chem Lett 15: 2093-6 (2005)
Ranbaxy Research Laboratories
Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport.
Bioorg Med Chem Lett 15: 2087-91 (2005)
Genzyme
2-(Arylmethyl)-3-substituted quinuclidines as selective alpha 7 nicotinic receptor ligands.
Bioorg Med Chem Lett 15: 2073-7 (2005)
Targacept
Inhibitory activities against topoisomerase I and II by isoaurostatin derivatives and their structure-activity relationships.
Bioorg Med Chem Lett 15: 2065-8 (2005)
Kumamoto University
A general carbometalation, three component coupling strategy for the synthesis of alpha,beta-unsaturated gamma-sultines including thio-rofecoxib, a selective COX-2 inhibitor.
Bioorg Med Chem Lett 15: 2057-60 (2005)
Methylgene
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett 15: 2041-5 (2005)
Merck Research Laboratories
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.
Bioorg Med Chem Lett 15: 2033-9 (2005)
Abbott Laboratories
Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.
Bioorg Med Chem Lett 15: 1997-2001 (2005)
Merck Research Laboratories
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
Bioorg Med Chem Lett 15: 1993-6 (2005)
Merck Research Laboratories
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
Bioorg Med Chem Lett 15: 1987-91 (2005)
Virginia Commonwealth University
Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 15: 1973-7 (2005)
Bayer Research Center
Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors.
Bioorg Med Chem Lett 15: 1969-72 (2005)
Miikana Therapeutics
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.
J Med Chem 48: 2695-700 (2005)
Biota
Anchor-GRIND: filling the gap between standard 3D QSAR and the GRid-INdependent descriptors.
J Med Chem 48: 2687-94 (2005)
Imim/Universitat Pompeu Fabra
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
J Med Chem 48: 2678-86 (2005)
Mitsubishi Pharma
Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists.
J Med Chem 48: 2646-54 (2005)
D'Annunzio University of Chieti���Pescara
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.
J Med Chem 48: 2638-45 (2005)
University of Sassari
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
J Med Chem 48: 2627-37 (2005)
University Walk
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.
J Med Chem 48: 2559-70 (2005)
Columbia University College of Physicians and Surgeons
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.
J Med Chem 48: 2548-2558 (2005)
TBA
Virtual screening workflow development guided by the"receiver operating characteristic" curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4.
J Med Chem 48: 2534-47 (2005)
Paris Descartes University
Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation.
J Med Chem 48: 2509-17 (2005)
Université
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.
J Med Chem 48: 2493-508 (2005)
Friedrich-Alexander University
Architecture of the human urotensin II receptor: comparison of the binding domains of peptide and non-peptide urotensin II agonists.
J Med Chem 48: 2480-92 (2005)
Università
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
J Med Chem 48: 2469-79 (2005)
Molecular Discovery
LEA3D: a computer-aided ligand design for structure-based drug design.
J Med Chem 48: 2457-68 (2005)
University of Montpellier
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.
J Med Chem 48: 2420-31 (2005)
Università
Sulfur-substituted alpha-alkyl phenethylamines as selective and reversible MAO-A inhibitors: biological activities, CoMFA analysis, and active site modeling.
J Med Chem 48: 2407-19 (2005)
Universidad De Chile
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.
J Med Chem 48: 2388-406 (2005)
Pfizer
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.
J Med Chem 48: 2371-87 (2005)
Pfizer
Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.
J Med Chem 48: 2336-45 (2005)
Decode Biostructures
Enantiospecificity of glutamate carboxypeptidase II inhibition.
J Med Chem 48: 2319-24 (2005)
Guilford Pharmaceuticals
9-hydroxyazafluorenes and their use in thrombin inhibitors.
J Med Chem 48: 2282-93 (2005)
Merck Research Laboratories
Virtual docking approaches to protein kinase B inhibition.
J Med Chem 48: 2278-81 (2005)
The Burnham Institute
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.
J Med Chem 48: 2274-7 (2005)
Schering-Plough Research Institute
Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.
J Med Chem 48: 2270-3 (2005)
Eli Lilly
3-Substituted imidazo[1,2-d][1,2,4]-thiadiazoles: a novel class of factor XIIIa inhibitors.
J Med Chem 48: 2266-9 (2005)
Apotex Research
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
J Med Chem 48: 2262-5 (2005)
Merck Research Laboratories
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
J Med Chem 48: 2258-61 (2005)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.
J Pharmacol Exp Ther 314: 244-51 (2005)
Kyowa Hakko Kogyo
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
J Biol Chem 280: 21847-53 (2005)
University of Texas Southwestern Medical Center
Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera.
J Nat Prod 68: 447-9 (2005)
Chiba University
Terphenylquinone inhibitors of the src protein tyrosine kinase from Stilbella sp.
J Nat Prod 68: 323-6 (2005)
Boehringer Ingelheim Pharma
Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes.
J Pharmacol Exp Ther 314: 191-200 (2005)
Abbott Laboratories
UDP-glucuronosyltransferases and clinical drug-drug interactions.
Pharmacol Ther 106: 97-132 (2005)
The University of British Columbia
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.
Bioorg Med Chem Lett 15: 1943-7 (2005)
Eli Lilly
Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II.
Bioorg Med Chem Lett 15: 1937-42 (2005)
University of Naples 'Federico Ii
Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.
Bioorg Med Chem Lett 15: 1931-5 (2005)
University of Auckland
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides.
Bioorg Med Chem Lett 15: 1909-13 (2005)
Università
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.
Bioorg Med Chem Lett 15: 1901-7 (2005)
Merck Research Laboratories
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Bioorg Med Chem Lett 15: 1895-9 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors.
Bioorg Med Chem Lett 15: 1891-4 (2005)
Wyeth Research
Structure-activity relationship study of novel tissue transglutaminase inhibitors.
Bioorg Med Chem Lett 15: 1885-9 (2005)
Harvard Medical School
Synthesis of 15R-PGD2: a potential DP2 receptor agonist.
Bioorg Med Chem Lett 15: 1873-6 (2005)
Florida Institute of Technology
Structure-based design of derivatives of tyropeptin A as the potent and selective inhibitors of mammalian 20S proteasome.
Bioorg Med Chem Lett 15: 1867-71 (2005)
Numazu Bio-Medical Research Institute
Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists.
Bioorg Med Chem Lett 15: 1857-61 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
Bioorg Med Chem Lett 15: 1847-50 (2005)
Lanzhou University
1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors.
Bioorg Med Chem Lett 15: 1841-5 (2005)
Chemical Diversity Research Institute
Novel heterocyclic thyromimetics.
Bioorg Med Chem Lett 15: 1835-40 (2005)
Bayer Healthcare
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
Bioorg Med Chem Lett 15: 1829-33 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.
Bioorg Med Chem Lett 15: 1815-9 (2005)
Glaxosmithkline
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Bioorg Med Chem Lett 15: 1807-10 (2005)
Pfizer
Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.
Bioorg Med Chem Lett 15: 1799-802 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.
Bioorg Med Chem Lett 15: 1793-7 (2005)
National Institute of Pharmaceutical Education and Research (NIPER)
Structure-activity relationships of the oxindole growth hormone secretagogues.
Bioorg Med Chem Lett 15: 1789-92 (2005)
Sumitomo Pharmaceuticals
QSAR-by-NMR: quantitative insights into structural determinants for binding affinity by analysis of 1H/15N chemical shift differences in MMP-3 ligands.
Bioorg Med Chem Lett 15: 1779-83 (2005)
Aventis Pharma Deutschland
18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
Bioorg Med Chem Lett 15: 1773-7 (2005)
Technische Universit£T M£Nchen
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
J Biol Chem 280: 19867-74 (2005)
Berlex Biosciences
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
J Med Chem 48: 2248-50 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.
J Med Chem 48: 2243-7 (2005)
Glaxosmithkline Research & Development
Development of low molecular weight HIV-1 protease dimerization inhibitors.
J Med Chem 48: 2239-42 (2005)
Purdue University
4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.
J Med Chem 48: 2229-38 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
J Med Chem 48: 2194-211 (2005)
Pharmaceutical Research Institute
Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines.
J Med Chem 48: 2154-66 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.
J Med Chem 48: 2134-53 (2005)
Janssen-Cilag
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
J Med Chem 48: 2126-33 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
J Med Chem 48: 2121-5 (2005)
Universita Degli Studi Di Firenze
Development of spin-labeled probes for adenosine receptors.
J Med Chem 48: 2108-14 (2005)
University of Bonn
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
J Med Chem 48: 2100-7 (2005)
Vrije Universiteit Amsterdam
Synthesis of new benzoxazinone derivatives as neuropeptide Y5 antagonists for the treatment of obesity.
J Med Chem 48: 2080-92 (2005)
Laboratorios Dr. Esteve
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
J Med Chem 48: 2054-71 (2005)
Janssen-Cilag
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
J Med Chem 48: 2045-53 (2005)
Leiden/Amsterdam Center For Drug Research
Biological properties of D- and L-1-deoxyazasugars.
J Med Chem 48: 2036-44 (2005)
Toyama Medical and Pharmaceutical University
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.
J Med Chem 48: 2026-35 (2005)
University of Ferrara
Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
J Med Chem 48: 2009-18 (2005)
Biogen Idec
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
J Med Chem 48: 1984-2008 (2005)
Johnson & Johnson Pharmaceutical
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
J Med Chem 48: 1965-73 (2005)
Tibotec
Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform.
J Med Chem 48: 1941-7 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase.
J Med Chem 48: 1930-40 (2005)
Tibotec
Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.
J Med Chem 48: 1919-29 (2005)
Universita Di Siena
Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.
J Med Chem 48: 1886-900 (2005)
Johnson & Johnson Pharmaceutical
Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
J Med Chem 48: 1873-85 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
J Med Chem 48: 1857-72 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
J Med Chem 48: 1849-56 (2005)
The Scripps Research Institute
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
J Med Chem 48: 1839-48 (2005)
University of Arizona
Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists.
J Med Chem 48: 1823-38 (2005)
Solvay Pharma
Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.
J Med Chem 48: 1806-12 (2005)
University of Kansas
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
J Med Chem 48: 1796-805 (2005)
Saarland University
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
J Med Chem 48: 1781-95 (2005)
Laboratorios Dr. Esteve
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.
J Med Chem 48: 1768-80 (2005)
University of Antwerp
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
J Med Chem 48: 1745-58 (2005)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
J Med Chem 48: 1729-44 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.
J Med Chem 48: 1725-8 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
J Med Chem 48: 1721-4 (2005)
University of Illinois At Chicago
2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.
J Med Chem 48: 1717-20 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
J Med Chem 48: 1709-12 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
J Med Chem 48: 1705-8 (2005)
Università
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.
J Med Chem 48: 1701-4 (2005)
Universitat De Barcelona
Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor.
J Med Chem 48: 1697-700 (2005)
Research and Development
Desensitization of the human motilin receptor by motilides.
J Pharmacol Exp Ther 313: 1397-405 (2005)
Katholieke Universiteit Leuven
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.
Bioorg Med Chem 13: 2665-78 (2005)
Biocryst Pharmaceuticals
Discovery of novel non-peptidic ketopiperazine-based renin inhibitors.
Bioorg Med Chem 13: 2657-64 (2005)
Pfizer
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
Bioorg Med Chem Lett 15: 1749-53 (2005)
Athersys
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.
Bioorg Med Chem Lett 15: 1743-7 (2005)
Wyeth-Ayerst Research
A two-state homology model of the hERG K+ channel: application to ligand binding.
Bioorg Med Chem Lett 15: 1737-41 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel beta-(imidazol-4-yl)-beta-amino acids: solid-phase synthesis and study of their inhibitory activity against geranylgeranyl protein transferase type I.
Bioorg Med Chem Lett 15: 1713-9 (2005)
Janssen Research Foundation
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands.
Bioorg Med Chem Lett 15: 1707-11 (2005)
Virginia Commonwealth University
Design, synthesis and structure-activity relationship studies of hexahydropyrazinoquinolines as a novel class of potent and selective dopamine receptor 3 (D3) ligands.
Bioorg Med Chem Lett 15: 1701-5 (2005)
University of Michigan
Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.
Bioorg Med Chem Lett 15: 1697-700 (2005)
Roche Palo Alto
Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors.
Bioorg Med Chem Lett 15: 1687-91 (2005)
Johnson and Johnson Pharmaceutical Research and Development
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
Bioorg Med Chem Lett 15: 1683-6 (2005)
University of Montpellier
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.
Bioorg Med Chem Lett 15: 1675-81 (2005)
Merck Research Laboratories
Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs).
Bioorg Med Chem Lett 15: 1669-73 (2005)
Osi Pharmaceuticals
Combinatorial approaches towards the discovery of new tryptase inhibitors.
Bioorg Med Chem Lett 15: 1659-64 (2005)
University of Barcelona
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.
Bioorg Med Chem Lett 15: 1647-50 (2005)
Merck Research Laboratories
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.
Bioorg Med Chem Lett 15: 1641-5 (2005)
Wyeth Research
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Bioorg Med Chem Lett 15: 1623-7 (2005)
Amgen
Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs).
Bioorg Med Chem Lett 15: 1619-21 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel and potent NPY5 receptor antagonists derived from virtual screening and iterative parallel chemistry design.
Bioorg Med Chem Lett 15: 1599-603 (2005)
F. Hoffmann-La Roche
Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Bioorg Med Chem Lett 15: 1587-90 (2005)
Pfizer
Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Bioorg Med Chem Lett 15: 1583-6 (2005)
Human Biomolecular Research Institute
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.
Bioorg Med Chem Lett 15: 1577-82 (2005)
Abbott Laboratories
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.
Bioorg Med Chem Lett 15: 1565-71 (2005)
Merck Research Laboratories
3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis.
Bioorg Med Chem Lett 15: 1557-60 (2005)
Nps Pharmaceuticals
Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture.
Bioorg Med Chem Lett 15: 1553-6 (2005)
Glaxosmithkline
Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states.
J Pharmacol Exp Ther 313: 1281-8 (2005)
Neurocrine Biosciences
Endocrinological properties of two novel nonsteroidal progesterone receptor modulators, CP8816 and CP8863.
J Pharmacol Exp Ther 313: 916-20 (2005)
Meiji Seika Kaisha
Identification of small molecule chemical inhibitors of the collagen-specific chaperone Hsp47.
J Med Chem 48: 1680-4 (2005)
Mcmaster University
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.
J Med Chem 48: 1676-9 (2005)
University of Bath
Discovery of a novel class of reversible non-peptide caspase inhibitors via a structure-based approach.
J Med Chem 48: 1649-56 (2005)
Burnham Institute
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.
J Med Chem 48: 1620-9 (2005)
University of Medicine & Dentistry of New Jersey-Robert Wood Johnson Medical School (Umdnj-Rwjms)
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
J Med Chem 48: 1610-9 (2005)
Glaxosmithkline
Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.
J Med Chem 48: 1596-609 (2005)
Quorex Pharmaceuticals
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
J Med Chem 48: 1563-75 (2005)
Saarland University
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.
J Med Chem 48: 1550-62 (2005)
University of Camerino
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.
J Med Chem 48: 1540-9 (2005)
Neurocrine Biosciences
Design and biological evaluation of linear and cyclic phosphopeptide ligands of the N-terminal SH2 domain of protein tyrosine phosphatase SHP-1.
J Med Chem 48: 1528-39 (2005)
Friedrich-Schiller-University
Novel ligands for the chemokine receptor-3 (CCR3): a receptor-modeling study based on 5D-QSAR.
J Med Chem 48: 1515-27 (2005)
Biographics Laboratory 3R
NMR studies reveal structural differences between the gallium and yttrium complexes of DOTA-D-Phe1-Tyr3-octreotide.
J Med Chem 48: 1506-14 (2005)
Technische Universit£T M£Nchen
Dynamic receptor-based pharmacophore model development and its application in designing novel HIV-1 integrase inhibitors.
J Med Chem 48: 1496-505 (2005)
University of Houston
A shape-based 3-D scaffold hopping method and its application to a bacterial protein-protein interaction.
J Med Chem 48: 1489-95 (2005)
Wyeth Research
CoMFA and CoMSIA analyses of Pneumocystis carinii dihydrofolate reductase, Toxoplasma gondii dihydrofolate reductase, and rat liver dihydrofolate reductase.
J Med Chem 48: 1448-69 (2005)
Duquesne University
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
J Med Chem 48: 1421-7 (2005)
University of Ferrara
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
J Med Chem 48: 1367-83 (2005)
Merck Sharp & Dohme Research Laboratories
Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.
J Med Chem 48: 1359-66 (2005)
Kirin Brewery
Synthesis and biological evaluation of meperidine analogues at monoamine transporters.
J Med Chem 48: 1336-43 (2005)
University of New Orleans
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
J Med Chem 48: 1318-21 (2005)
Abbott Laboratories
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.
J Med Chem 48: 1314-7 (2005)
Irbm (Merck Research Laboratories Rome)
New approaches toward anti-HIV chemotherapy.
J Med Chem 48: 1297-313 (2005)
Katholieke Universiteit Leuven
From the insoluble dye indirubin towards highly active, soluble CDK2-inhibitors.
Chembiochem 6: 531-40 (2005)
Schering
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
Chem Biol 12: 237-47 (2005)
National Institutes of Health
Structural basis for the highly selective inhibition of MMP-13.
Chem Biol 12: 181-9 (2005)
Aventis Pharma Deutschland
Bioactive constituents from Boswellia papyrifera.
J Nat Prod 68: 189-93 (2005)
University of Karachi
Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.
J Am Chem Soc 127: 2741-51 (2005)
University of North Carolina
Use of binding enthalpy to drive an allosteric transition.
Biochemistry 44: 3112-21 (2005)
University of Maryland
CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.
J Med Chem 48: 1278-81 (2005)
Vertex Pharmaceuticals
Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter.
J Med Chem 48: 1274-7 (2005)
University of Michigan
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors.
J Med Chem 48: 1237-43 (2005)
Purdue Pharma
Chiral DNA gyrase inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl- 2H-benzo[a]quinolizin-20-one-3-carboxylic acid analogues.
J Med Chem 48: 1229-36 (2005)
University of Kansas
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists.
J Med Chem 48: 1221-8 (2005)
Research Triangle Institute
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.
J Med Chem 48: 1169-78 (2005)
Neurocrine Biosciences
Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action.
J Med Chem 48: 1145-51 (2005)
Leiden/Amsterdam Center For Drug Research
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
J Med Chem 48: 1107-31 (2005)
Wyeth Research
Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery.
J Med Chem 48: 1098-106 (2005)
University of Southern California
Structure-based drug discovery using GPCR homology modeling: successful virtual screening for antagonists of the alpha1A adrenergic receptor.
J Med Chem 48: 1088-97 (2005)
Aventis Pharma Deutschland
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
J Med Chem 48: 1019-32 (2005)
Nagoya City University
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
J Med Chem 48: 986-94 (2005)
National Institute On Aging
Application of a flexible synthesis of (5R)-thiolactomycin to develop new inhibitors of type I fatty acid synthase.
J Med Chem 48: 946-61 (2005)
Johns Hopkins University
Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core.
J Med Chem 48: 926-34 (2005)
Johnson and Johnson Pharmaceutical Research & Development
Three-dimensional structure-activity relationships of nonsteroidal ligands in complex with androgen receptor ligand-binding domain.
J Med Chem 48: 917-25 (2005)
Csc-Scientific Computing
Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine.
J Med Chem 48: 913-6 (2005)
Università
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
J Med Chem 48: 909-12 (2005)
Johnson & Johnson Pharmaceutical
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors.
J Med Chem 48: 905-8 (2005)
Pfizer
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
J Med Chem 48: 897-900 (2005)
7Tm Pharma
(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors.
Bioorg Med Chem Lett 15: 1525-7 (2005)
National Research Laboratory of Lipid Metabolism and Atherosclerosis
Lysine derivatives as potent HIV protease inhibitors. Discovery, synthesis and structure-activity relationship studies.
Bioorg Med Chem Lett 15: 1509-13 (2005)
Pharmacor
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.
Bioorg Med Chem Lett 15: 1505-7 (2005)
Chinese Academy of Sciences
Glucokinase-activating ureas.
Bioorg Med Chem Lett 15: 1501-4 (2005)
Osi Pharmaceuticals
Structure-activity relationships of dimeric PPAR agonists.
Bioorg Med Chem Lett 15: 1497-500 (2005)
Novo Nordisk
Aglycon specificity profiling of alpha-glucosidases using synthetic probes.
Bioorg Med Chem Lett 15: 1489-92 (2005)
Institute of Physical and Chemical Research (Riken)
Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles.
Bioorg Med Chem Lett 15: 1475-8 (2005)
Genomics Institute of The Novartis Research Foundation
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.
Bioorg Med Chem Lett 15: 1467-70 (2005)
Arena Pharmaceuticals
Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.
Bioorg Med Chem Lett 15: 1463-6 (2005)
Ligand Pharmaceuticals
Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors.
Bioorg Med Chem Lett 15: 1457-61 (2005)
Queen'S University
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.
Bioorg Med Chem Lett 15: 1441-6 (2005)
Merck Research Laboratories
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.
Bioorg Med Chem Lett 15: 1435-40 (2005)
Bristol-Myers Squibb
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.
Bioorg Med Chem Lett 15: 1429-33 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity.
Bioorg Med Chem Lett 15: 1423-8 (2005)
The Scripps Research Institute
Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.
Bioorg Med Chem Lett 15: 1407-11 (2005)
Neurocrine Biosciences
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Bioorg Med Chem Lett 15: 1401-5 (2005)
Merck Research Laboratories
Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic.
Bioorg Med Chem Lett 15: 1385-8 (2005)
Nih
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.
Bioorg Med Chem Lett 15: 1379-83 (2005)
Maxim Pharmaceuticals
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.
Bioorg Med Chem Lett 15: 1375-8 (2005)
Schering-Plough Research Institute
Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives.
Bioorg Med Chem Lett 15: 1361-6 (2005)
Dainippon Pharmaceutical
(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.
Bioorg Med Chem Lett 15: 1345-9 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.
Bioorg Med Chem Lett 15: 1337-40 (2005)
Korea Research Institute of Chemical Technology
cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.
Bioorg Med Chem Lett 15: 1327-31 (2005)
Amura Therapeutics
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
Bioorg Med Chem Lett 15: 1321-6 (2005)
University of Pisa
Benzodipyrazoles: a new class of potent CDK2 inhibitors.
Bioorg Med Chem Lett 15: 1315-9 (2005)
Nerviano Medical Sciences
Amino acid conjugates as kappa opioid receptor agonists.
Bioorg Med Chem Lett 15: 1279-82 (2005)
Adolor
A small molecule-kinase interaction map for clinical kinase inhibitors.
Nat Biotechnol 23: 329-36 (2005)
Ambit Biosciences
Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors.
J Biol Chem 280: 15761-6 (2005)
Emory University
Structure-aided optimization of kinase inhibitors derived from alsterpaullone.
Chembiochem 6: 541-9 (2005)
Technische UniversitÄT Braunschweig
Inhibition of angiogenesis-relevant receptor tyrosine kinases by sulindac analogues.
Chembiochem 6: 527-31 (2005)
Max-Planck-Institut FÜR Molekulare Physiologie
Carbocyclic[g]indole inhibitors of human nonpancreatic s-PLA2.
J Med Chem 48: 893-6 (2005)
Eli Lilly
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
J Med Chem 48: 849-56 (2005)
Unibioscreen
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
J Med Chem 48: 839-48 (2005)
National Institute On Drug Abuse-Intramural Research Program
Design and synthesis of conformationally constrained Grb2 SH2 domain binding peptides employing alpha-methylphenylalanyl based phosphotyrosyl mimetics.
J Med Chem 48: 764-72 (2005)
National Cancer Institute-Frederick
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
J Med Chem 48: 744-52 (2005)
Abbott Laboratories
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.
J Med Chem 48: 737-43 (2005)
Lawrence Berkeley National Laboratory
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
J Med Chem 48: 694-709 (2005)
Friedrich-Alexander University
Mechanism of CDK5/p25 binding by CDK inhibitors.
J Med Chem 48: 671-9 (2005)
European Institute of Oncology
Alkylamino derivatives of 4-aminomethylpyridine as inhibitors of copper-containing amine oxidases.
J Med Chem 48: 664-70 (2005)
University of Genoa
Structure of human cytidine deaminase bound to a potent inhibitor.
J Med Chem 48: 658-60 (2005)
Harvard University
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.
J Med Chem 48: 655-7 (2005)
Shanghai Institute of Materia Medica
N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase.
Bioorg Med Chem Lett 15: 1235-8 (2005)
Novartis Institutes For Biomedical Research
Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.
Bioorg Med Chem Lett 15: 1225-8 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 15: 1221-4 (2005)
National Institute of Diabetes and Digestive and Kidney Diseases
1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.
Bioorg Med Chem Lett 15: 1217-20 (2005)
Novartis Institutes For Biomedical Research
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Bioorg Med Chem Lett 15: 1201-4 (2005)
Abbott Laboratories
Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Bioorg Med Chem Lett 15: 1197-200 (2005)
Merck Research Laboratories
1,2,4-Benzothiadiazine derivatives as alpha1 and 5-HT1A receptor ligands.
Bioorg Med Chem Lett 15: 1185-8 (2005)
University of Modena and Reggio Emilia
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Bioorg Med Chem Lett 15: 1173-80 (2005)
Merck Frosst Centre For Therapeutic Research
Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists.
Bioorg Med Chem Lett 15: 1165-7 (2005)
RhôNe-Poulenc Rorer
De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.
Bioorg Med Chem Lett 15: 1161-4 (2005)
Cerep
2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Bioorg Med Chem Lett 15: 1155-60 (2005)
Merck Frosst Centre For Therapeutic Research
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Bioorg Med Chem Lett 15: 1149-54 (2005)
Universita Degli Studi Di Firenze
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.
Bioorg Med Chem Lett 15: 1143-7 (2005)
University of Kansas
Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status.
Bioorg Med Chem Lett 15: 1135-8 (2005)
Mcgill University/Royal Victoria Hospital
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.
Bioorg Med Chem Lett 15: 1131-3 (2005)
Yale University
Reversal of anticancer drug resistance by COTC based on intracellular glutathione and glyoxalase I.
Bioorg Med Chem Lett 15: 1111-4 (2005)
Keio University
Human immunodeficiency virus-reverse transcriptase inhibition and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of fullerene derivatives.
Bioorg Med Chem Lett 15: 1107-9 (2005)
Kyoritsu University of Pharmacy
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
Bioorg Med Chem Lett 15: 1101-6 (2005)
Pharmaceutical Research Institute
Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists.
Bioorg Med Chem Lett 15: 1091-5 (2005)
Adolor
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
Bioorg Med Chem Lett 15: 1083-5 (2005)
Ucb Pharma
Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.
Bioorg Med Chem Lett 15: 1061-4 (2005)
Dainippon Pharmaceutical
Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.
Bioorg Med Chem Lett 15: 1055-9 (2005)
Dainippon Pharmaceutical
Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata.
Bioorg Med Chem Lett 15: 1051-4 (2005)
Hokkaido University
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).
Bioorg Med Chem Lett 15: 1027-32 (2005)
National Institute of Pharmaceutical Education and Research (NIPER)
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.
Bioorg Med Chem Lett 15: 999-1004 (2005)
Neurocrine Biosciences
Two new irreversible inhibitors of dihydrodipicolinate synthase: diethyl (E,E)-4-oxo-2,5-heptadienedioate and diethyl (E)-4-oxo-2-heptenedioate.
Bioorg Med Chem Lett 15: 995-8 (2005)
University of Sydney
Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase.
Bioorg Med Chem Lett 15: 989-94 (2005)
Universidad Nacional AutóNoma De MéXico
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.
Bioorg Med Chem Lett 15: 977-82 (2005)
Merck Research Laboratories
Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides.
Bioorg Med Chem Lett 15: 971-6 (2005)
Universita Degli Studi Di Firenze
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
Bioorg Med Chem Lett 15: 963-9 (2005)
Universita Degli Studi Di Firenze
QSAR of estrogen receptor modulators: exploring selectivity requirements for ER(alpha) versus ER(beta) binding of tetrahydroisoquinoline derivatives using E-state and physicochemical parameters.
Bioorg Med Chem Lett 15: 957-61 (2005)
University of Calcutta
A rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by 1,n-alkane-di-N-butylcarbamates.
Bioorg Med Chem Lett 15: 951-5 (2005)
National Chung-Hsing University
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.
Bioorg Med Chem Lett 15: 945-9 (2005)
Yale University
Studies towards the next generation of antidepressants. Part 4: derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor.
Bioorg Med Chem Lett 15: 911-4 (2005)
Wyeth Research
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
Bioorg Med Chem Lett 15: 905-9 (2005)
Merck Research Laboratories
The development of potent and selective bisarylmaleimide GSK3 inhibitors.
Bioorg Med Chem Lett 15: 899-903 (2005)
Lilly Research Laboratories
6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model.
Bioorg Med Chem Lett 15: 877-81 (2005)
University of California
4'C-ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 15: 869-71 (2005)
Universit£T Konstanz
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.
Bioorg Med Chem Lett 15: 863-7 (2005)
Vernalis (R&D)
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design.
Nat Biotechnol 23: 201-7 (2005)
Plexxikon
Lanostane triterpenoids and triterpene glycosides from the fruit body of Fomitopsis pinicola and their inhibitory activity against COX-1 and COX-2.
J Nat Prod 68: 69-73 (2005)
Tokushima Bunri University
Potent CYP3A4 inhibitory constituents of Piper cubeba.
J Nat Prod 68: 64-8 (2005)
Toyama Medical and Pharmaceutical University
Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog.
J Pharmacol Exp Ther 313: 1101-8 (2005)
Mayo Clinic
Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists.
J Pharmacol Exp Ther 313: 831-9 (2005)
Taisho Pharmaceutical
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.
Bioorg Med Chem 13: 949-61 (2005)
Yamanouchi Pharmaceutical
Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2.
J Pharmacol Exp Ther 313: 549-56 (2005)
German Cancer Research Center
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.
Bioorg Med Chem Lett 15: 833-7 (2005)
Neurocrine Biosciences
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.
Bioorg Med Chem Lett 15: 823-5 (2005)
Martin-Luther-University Halle-Wittenberg
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Bioorg Med Chem Lett 15: 817-22 (2005)
F. Hoffmann-La Roche
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides.
Bioorg Med Chem Lett 15: 805-7 (2005)
Kyoto 619-0216
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides.
Bioorg Med Chem Lett 15: 799-803 (2005)
Kyoto 619-0216
Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
Bioorg Med Chem Lett 15: 793-7 (2005)
University of Michigan
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists.
Bioorg Med Chem Lett 15: 787-91 (2005)
Dbristol-Myers Squibb
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Bioorg Med Chem Lett 15: 783-6 (2005)
Schering-Plough Research Institute
Non-peptidic small molecule inhibitors of XIAP.
Bioorg Med Chem Lett 15: 771-5 (2005)
Abbott Laboratories
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Bioorg Med Chem Lett 15: 761-4 (2005)
Merck Research Laboratories
Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
Bioorg Med Chem Lett 15: 751-4 (2005)
Celltech R and D
Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.
Bioorg Med Chem Lett 15: 747-50 (2005)
Uppsala University
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Bioorg Med Chem Lett 15: 737-41 (2005)
Glaxosmithkline
Active site directed inhibitors of replication-specific bacterial DNA polymerases.
Bioorg Med Chem Lett 15: 729-32 (2005)
Glsynthesis
4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists.
Bioorg Med Chem Lett 15: 719-23 (2005)
Purdue Pharma
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
Bioorg Med Chem Lett 15: 715-8 (2005)
Merck Research Laboratories
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.
Bioorg Med Chem Lett 15: 693-8 (2005)
Neurocrine Biosciences
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
Bioorg Med Chem Lett 15: 687-91 (2005)
National Health Research Institutes
Parallel synthesis of pteridine derivatives as potent inhibitors for hepatitis C virus NS5B RNA-dependent RNA polymerase.
Bioorg Med Chem Lett 15: 675-8 (2005)
Valeant Pharmaceuticals International
Pyrrolidinohydroquinazolines--a novel class of CCR3 modulators.
Bioorg Med Chem Lett 15: 669-73 (2005)
Boehringer Ingelheim Pharma Gmbh And
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
Bioorg Med Chem Lett 15: 657-64 (2005)
China Pharmaceutical University
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.
Bioorg Med Chem Lett 15: 645-51 (2005)
Merck Research Laboratories
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold.
Bioorg Med Chem Lett 15: 635-8 (2005)
Chinese Academy of Sciences
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands.
Bioorg Med Chem Lett 15: 631-4 (2005)
Seoul National University
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.
Bioorg Med Chem Lett 15: 609-12 (2005)
Cv Therapeutics
Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).
Bioorg Med Chem Lett 15: 599-602 (2005)
Kobe Gakuin University
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
Bioorg Med Chem Lett 15: 589-93 (2005)
Organon Laboratories
Generation of a new class of hNK(2) receptor ligands using the 'fragment approach'.
Bioorg Med Chem Lett 15: 585-8 (2005)
Menarini Ricerche
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
Bioorg Med Chem Lett 15: 579-84 (2005)
Universita Degli Studi Di Firenze
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates.
Bioorg Med Chem Lett 15: 573-8 (2005)
Università
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate.
Bioorg Med Chem Lett 15: 567-71 (2005)
Universita Degli Studi Di Firenze
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
Bioorg Med Chem Lett 15: 527-30 (2005)
Merck Frosst Centre For Therapeutic Research
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
Bioorg Med Chem Lett 15: 523-6 (2005)
Chinese Academy of Sciences
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.
Bioorg Med Chem Lett 15: 511-5 (2005)
Biogen Idec
Enhanced ligand affinity for receptors in which components of the binding site are independently mobile.
Chem Biol 12: 89-97 (2005)
University of Sheffield
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.
Chem Biol 12: 65-76 (2005)
University of Dundee
Synthesis and biological evaluation of thienopyrrolizines, a new family of CDK/GSK-3 inhibitors.
J Enzyme Inhib Med Chem 19: 585-93 (2004)
UniversitÉ
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.
J Med Chem 48: 586-92 (2005)
Kobe Gakuin University
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.
J Med Chem 48: 569-85 (2005)
Newcastle University
Further naphthylcombretastatins. An investigation on the role of the naphthalene moiety.
J Med Chem 48: 556-68 (2005)
Universidad De Salamanca
Sulfonamide drugs binding to the colchicine site of tubulin: thermodynamic analysis of the drug-tubulin interactions by isothermal titration calorimetry.
J Med Chem 48: 547-55 (2005)
Institute
Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
J Med Chem 48: 515-22 (2005)
Salk Institute
Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
J Med Chem 48: 507-14 (2005)
Salk Institute
Identification of 4-substituted 1,2,3-triazoles as novel oxazolidinone antibacterial agents with reduced activity against monoamine oxidase A.
J Med Chem 48: 499-506 (2005)
Astrazeneca Discovery
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
J Med Chem 48: 483-98 (2005)
University Institute of Pathology
Investigations on the effects of basic side chains on the hormonal profile of (4R,5S)/(4S,5R)-4,5-bis(4-hydroxyphenyl)-2-imidazolines.
J Med Chem 48: 466-74 (2005)
Free University of Berlin
Quantitative structure-activity relationship (5D-QSAR) study of combretastatin-like analogues as inhibitors of tubulin assembly.
J Med Chem 48: 457-65 (2005)
University of Salford
Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme.
J Med Chem 48: 440-9 (2005)
University of Kuopio
Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.
J Med Chem 48: 414-26 (2005)
Astex
Aminoimidazolylmethyluracil analogues as potent inhibitors of thymidine phosphorylase and their bioreductive nitroimidazolyl prodrugs.
J Med Chem 48: 392-402 (2005)
University of Manchester
Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131.
J Med Chem 48: 380-91 (2005)
Kyoto University
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
J Med Chem 48: 364-79 (2005)
Novartis Pharmaceuticals
Rational approach to discover multipotent anti-Alzheimer drugs.
J Med Chem 48: 360-3 (2005)
University of Bologna
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
J Med Chem 48: 353-6 (2005)
Wyeth Research
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.
J Med Chem 48: 345-8 (2005)
University of Melbourne
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002.
J Biol Chem 280: 13728-34 (2005)
Vertex Pharmaceuticals
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
Br J Pharmacol 144: 317-22 (2005)
University of Nottingham
Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'.
Bioorg Med Chem 13: 755-64 (2005)
Uppsala University
Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney.
Drug Metab Dispos 33: 495-9 (2005)
Tokyo University of Science
Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.
J Med Chem 48: 330-4 (2005)
Université
Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines.
J Med Chem 48: 321-9 (2005)
Leiden University
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
J Med Chem 48: 306-11 (2005)
Novo Nordisk
Structure-activity relationships and effects on neuroactive steroid synthesis in a series of 2-phenylimidazo[1,2-a]pyridineacetamide peripheral benzodiazepine receptors ligands.
J Med Chem 48: 292-305 (2005)
Università
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators.
J Med Chem 48: 287-91 (2005)
Institut Claudius Regaud
Design and NMR characterization of active analogues of compstatin containing non-natural amino acids.
J Med Chem 48: 274-86 (2005)
University of California Riverside
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
J Med Chem 48: 266-73 (2005)
University of Modena and Reggio Emilia
Discovery of corticotropin releasing factor 2 receptor selective sauvagine analogues for treatment of skeletal muscle atrophy.
J Med Chem 48: 262-5 (2005)
Procter & Gamble Pharmaceuticals
5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6.
J Med Chem 48: 224-39 (2005)
Human Biomolecular Research Institute
Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.
J Med Chem 48: 163-70 (2005)
Max-Planck-Institut Fuer Biochemie
Combined target-based and ligand-based drug design approach as a tool to define a novel 3D-pharmacophore model of human A3 adenosine receptor antagonists: pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as a key study.
J Med Chem 48: 152-62 (2005)
Università
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
J Med Chem 48: 141-51 (2005)
Merck Research Laboratories
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
J Med Chem 48: 134-40 (2005)
University of Kansas
Beta-diketo acid pharmacophore hypothesis. 1. Discovery of a novel class of HIV-1 integrase inhibitors.
J Med Chem 48: 111-20 (2005)
University of Southern California
Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.
J Med Chem 48: 100-10 (2005)
National Center For Scientific Research Demokritos
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
J Med Chem 48: 71-90 (2005)
Amgen
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
J Med Chem 48: 38-55 (2005)
Abbott Laboratories
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
J Med Chem 48: 24-7 (2005)
University of Bologna
Control of hepatitis C: a medicinal chemistry perspective.
J Med Chem 48: 1-20 (2005)
University of Wollongong
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
J Biol Chem 280: 9160-9 (2005)
Genentech
In vitro and in vivo pharmacological characterization of BM-613 [N-n-pentyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist.
J Pharmacol Exp Ther 313: 293-301 (2005)
University of Li&Eagrove;Ge
Meroterpenoid MAPKAP (MK2) inhibitors isolated from the indonesian marine sponge Acanthodendrilla sp.
J Nat Prod 67: 2127-9 (2004)
University of British Columbia
A phthalide with in vitro growth inhibitory activity from an oidiodendron strain.
J Nat Prod 67: 2086-9 (2004)
Cetek
Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells.
J Nat Prod 67: 2002-7 (2004)
University of Mississippi
Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.
Drug Metab Pharmacokinet 17: 125-9 (2002)
Kyoto University Hospital
The potential for an interaction between MRP2 (ABCC2) and various therapeutic agents: probenecid as a candidate inhibitor of the biliary excretion of irinotecan metabolites.
Drug Metab Pharmacokinet 17: 23-33 (2002)
University of Tokyo
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.
Drug Metab Dispos 33: 537-46 (2005)
Pfizer
Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues.
J Med Chem 47: 6958-63 (2004)
Harvard Medical School
Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.
J Med Chem 47: 6948-57 (2004)
The Danish University of Pharmaceutical Sciences
Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.
J Med Chem 47: 6935-47 (2004)
Menarini Ricerche
Design, synthesis, and biological activity of novel, potent, and selective (benzoylaminomethyl)thiophene sulfonamide inhibitors of c-Jun-N-terminal kinase.
J Med Chem 47: 6921-34 (2004)
Serono Pharmaceutical Research Institute
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.
J Med Chem 47: 6893-901 (2004)
Duquesne University
A screening library for peptide activated G-protein coupled receptors. 1. The test set.
J Med Chem 47: 6864-74 (2004)
Neurocrine Biosciences
Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).
J Med Chem 47: 6854-63 (2004)
The Johns Hopkins University
4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.
J Med Chem 47: 6821-30 (2004)
Neurocrine Biosciences
Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors.
J Med Chem 47: 6792-803 (2004)
University of Bari
Charge and substituent effects on affinity and metabolism of benzbromarone-based CYP2C19 inhibitors.
J Med Chem 47: 6768-76 (2004)
Washington State University
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.
J Med Chem 47: 6749-59 (2004)
Université
Benzoyl ring halogenated classical 2-amino-6-methyl-3,4-dihydro-4-oxo-5-substituted thiobenzoyl-7H-pyrrolo[2,3-d]pyrimidine antifolates as inhibitors of thymidylate synthase and as antitumor agents.
J Med Chem 47: 6730-9 (2004)
Duquesne University
Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice.
J Med Chem 47: 6716-29 (2004)
University of Maryland
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
J Med Chem 47: 6702-10 (2004)
University of Florida
Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine.
J Med Chem 47: 6691-701 (2004)
Indian Institute of Technology
Virtual screening of human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase against the NCI diversity set by use of AutoDock to identify novel nonfolate inhibitors.
J Med Chem 47: 6681-90 (2004)
The Scripps Research Institute
A novel class of inhibitors of peptide deformylase discovered through high-throughput screening and virtual ligand screening.
J Med Chem 47: 6669-72 (2004)
Stine-Haskell Research Center
Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors.
J Med Chem 47: 6666-8 (2004)
Wyeth Research
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
J Med Chem 47: 6662-5 (2004)
Merck Research Laboratories
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
J Med Chem 47: 6658-61 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
J Med Chem 47: 6655-7 (2004)
Abbott Laboratories
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
J Pharmacol Exp Ther 313: 165-75 (2005)
Abbott Laboratories
5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Bioorg Med Chem Lett 15: 459-65 (2004)
Pfizer
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Bioorg Med Chem Lett 15: 447-51 (2004)
Merck Research Laboratories
Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme.
Bioorg Med Chem Lett 15: 439-42 (2004)
University of Alberta
Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis.
Bioorg Med Chem Lett 15: 431-4 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
3D QSAR studies on GSK-3 inhibition by aloisines.
Bioorg Med Chem Lett 15: 395-9 (2005)
Zhejiang University
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
Bioorg Med Chem Lett 15: 389-93 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors.
Bioorg Med Chem Lett 15: 385-8 (2004)
Korea Research Institute of Bioscience and Biotechnology
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 15: 379-83 (2004)
Wyeth Research
A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.
Bioorg Med Chem Lett 15: 373-8 (2004)
Merck Sharp & Dohme Research Laboratories
Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX.
Bioorg Med Chem Lett 15: 367-72 (2004)
Harran University
(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.
Bioorg Med Chem Lett 15: 363-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzoyl 2-methyl indoles as selective PPARgamma modulators.
Bioorg Med Chem Lett 15: 357-62 (2004)
Merck Research Laboratories
Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus.
Bioorg Med Chem Lett 15: 353-6 (2004)
Korea Research Institute of Bioscience and Biotechnology
(2S,1'S,2'R,3'R)-2(2'-Carboxy-3'-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors.
Bioorg Med Chem Lett 15: 349-51 (2004)
Eli Lilly
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.
Bioorg Med Chem Lett 15: 331-5 (2005)
Nagoya City University
QSAR studies on structurally similar 2-(4-methanesulfonylphenyl)pyran-4-ones as selective COX-2 inhibitors: a Hansch approach.
Bioorg Med Chem Lett 15: 313-20 (2004)
Devi Ahilya Vishwavidyalaya
Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.
Bioorg Med Chem Lett 15: 283-6 (2004)
Korea Institute of Science & Technology
The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors.
Bioorg Med Chem Lett 15: 277-81 (2004)
Athersys
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.
Bioorg Med Chem Lett 15: 271-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.
Bioorg Med Chem Lett 15: 251-4 (2004)
Fujisawa Pharmaceutical
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.
Bioorg Med Chem 13: 425-32 (2005)
Mitsubishi Pharma
Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.
J Pharmacol Exp Ther 313: 410-21 (2005)
I.G.B.M.C.
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.
J Med Chem 47: 6645-8 (2004)
University of Bath
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
J Med Chem 47: 6616-24 (2004)
Università
Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database.
J Med Chem 47: 6609-15 (2004)
University of Mississippi
Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors.
J Med Chem 47: 6603-8 (2004)
Wyeth Research
Design, synthesis and evaluation of a PLG tripeptidomimetic based on a pyridine scaffold.
J Med Chem 47: 6595-602 (2004)
G£Teborg University
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.
J Med Chem 47: 6584-94 (2004)
Boehringer Ingelheim (Canada)
Structure-activity relationship of 6-methylidene penems bearing tricyclic heterocycles as broad-spectrum beta-lactamase inhibitors: crystallographic structures show unexpected binding of 1,4-thiazepine intermediates.
J Med Chem 47: 6556-68 (2004)
Wyeth Research
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
J Med Chem 47: 6541-6 (2004)
University of Cagliary
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
J Med Chem 47: 6529-40 (2004)
Leiden/Amsterdam Center For Drug Research
Antiestrogen binding site and estrogen receptor mediate uptake and distribution of 4-hydroxytamoxifen-targeted doxorubicin-formaldehyde conjugate in breast cancer cells.
J Med Chem 47: 6509-18 (2004)
University of Colorado
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
J Med Chem 47: 6490-8 (2004)
University of Bologna
Stereochemical analysis of (hydroxyethyl)urea peptidomimetic inhibitors of gamma-secretase.
J Med Chem 47: 6485-9 (2004)
Harvard Medical School
Catecholic flavonoids acting as telomerase inhibitors.
J Med Chem 47: 6466-75 (2004)
Bu-Nerviano Medical Sciences
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
J Med Chem 47: 6455-8 (2004)
University of Illinois At Chicago
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
J Med Chem 47: 6447-50 (2004)
Merck Research Laboratories
The design and enzyme-bound crystal structure of indoline based peptidomimetic inhibitors of hepatitis C virus NS3 protease.
J Med Chem 47: 6443-6 (2004)
Mrl Rome
2,3-diaminopyridine bradykinin B1 receptor antagonists.
J Med Chem 47: 6439-42 (2004)
Merck Research Laboratories
Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis.
J Med Chem 47: 6435-8 (2004)
Wyeth Research
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases.
Bioorg Med Chem 13: 257-64 (2005)
University of Alabama At Birmingham
Synthesis and aminoacyl-tRNA synthetase inhibitory activity of aspartyl adenylate analogs.
Bioorg Med Chem 13: 69-75 (2005)
Crefsip
The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors.
Bioorg Med Chem 13: 59-68 (2005)
Pfizer
Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives.
Bioorg Med Chem Lett 15: 235-8 (2004)
University of North Carolina
2,3-Diphenylpropionic acids as potent VLA-4 antagonists.
Bioorg Med Chem Lett 15: 217-20 (2004)
Kaken Pharmaceutical
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
Bioorg Med Chem Lett 15: 211-5 (2004)
Kyoto Pharmaceutical University
Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.
Bioorg Med Chem Lett 15: 195-201 (2004)
Abbott Laboratories
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors.
Bioorg Med Chem Lett 15: 185-9 (2004)
Central Pharmaceutical Research Institute
N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.
Bioorg Med Chem Lett 15: 181-3 (2004)
Sejong University
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Bioorg Med Chem Lett 15: 171-5 (2004)
Merck Research Laboratories
Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase.
Bioorg Med Chem Lett 15: 159-62 (2004)
National Institute of Health Sciences
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Bioorg Med Chem Lett 15: 153-8 (2004)
Abbott Laboratories
Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5alpha-reductases 1 and 2.
Bioorg Med Chem Lett 15: 145-8 (2004)
Polo Scientifico Università
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties.
Bioorg Med Chem Lett 15: 135-8 (2004)
University of The Mediterranean
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core.
Bioorg Med Chem Lett 15: 125-8 (2004)
Abbott Laboratories
Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain.
Bioorg Med Chem Lett 15: 121-3 (2004)
University of California San Francisco
Aminothiazole inhibitors of HCV RNA polymerase.
Bioorg Med Chem Lett 15: 115-9 (2004)
Neogenesis Pharmaceuticals
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.
Bioorg Med Chem Lett 15: 107-13 (2004)
Merck Research Laboratories
Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase.
Bioorg Med Chem Lett 15: 103-6 (2004)
The Scripps Research Institute
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Bioorg Med Chem Lett 15: 93-8 (2004)
Abbott Laboratories
Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters.
Bioorg Med Chem Lett 15: 85-7 (2004)
Xenoport
Optimization of pyrrolidinone based HIV protease inhibitors.
Bioorg Med Chem Lett 15: 81-4 (2005)
Glaxosmithkline
2,3-Ethylene- and 2,3-trimethylene-bridged analogues of the group III metabotropic glutamate receptor ligand 2-amino-4-phosphonobutanoic acid.
Bioorg Med Chem Lett 15: 57-60 (2004)
University of Minnesota
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
Bioorg Med Chem Lett 15: 51-5 (2004)
Eli Lilly
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.
Bioorg Med Chem Lett 15: 41-5 (2004)
Daiichi Pharmaceutical
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Bioorg Med Chem Lett 15: 29-35 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.
Bioorg Med Chem Lett 15: 25-8 (2004)
Astrazeneca
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).
Bioorg Med Chem Lett 15: 15-20 (2005)
University of Illinois At Chicago
Structural basis for the activity of drugs that inhibit phosphodiesterases.
Structure 12: 2233-47 (2004)
Plexxikon
Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors.
J Nat Prod 67: 1882-5 (2004)
Instituto De Qu£Mica Da Universidade Estadual Paulista
Isolation of cytochrome P450 inhibitors from strawberry fruit, Fragaria ananassa.
J Nat Prod 67: 1839-41 (2004)
Kanazawa University
Estrogenic and anticarcinogenic properties of kurarinone, a lavandulyl flavanone from the roots of Sophora flavescens.
J Nat Prod 67: 1829-32 (2004)
Ghent University
Mechanism-based inactivation of COX-1 by red wine m-hydroquinones: a structure-activity relationship study.
J Nat Prod 67: 1777-82 (2004)
University of Pennsylvania School of Medicine
Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.
Eur J Pharm Biopharm 59: 17-24 (2004)
Biozentrum of The Martin-Luther-University Halle-Wittenberg
Discovery of novel phenolic antioxidants as inhibitors of vascular cell adhesion molecule-1 expression for use in chronic inflammatory diseases.
J Med Chem 47: 6420-32 (2004)
Atherogenics
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
J Med Chem 47: 6401-9 (2004)
Research Triangle Institute
New constrained"molecular tongs" designed to dissociate HIV-1 protease dimer.
J Med Chem 47: 6392-400 (2004)
Paris-Sud University
Synthesis of tropeines and allosteric modulation of ionotropic glycine receptors.
J Med Chem 47: 6384-91 (2004)
Hungarian Academy of Sciences
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
J Med Chem 47: 6363-72 (2004)
Merck Research Laboratories
Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.
J Med Chem 47: 6326-37 (2004)
RhôNe-Poulenc Rorer
Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position.
J Med Chem 47: 6311-25 (2004)
Eberhard-Karls-University TüBingen
An in silico approach to discovering novel inhibitors of human sirtuin type 2.
J Med Chem 47: 6292-8 (2004)
University of Kuopio
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
J Med Chem 47: 6283-91 (2004)
Bristol-Myers Squibb
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.
J Med Chem 47: 6255-69 (2004)
Wyeth Research
Acetylcholinesterase inhibitory activity of scopolin and scopoletin discovered by virtual screening of natural products.
J Med Chem 47: 6248-54 (2004)
Leopold-Franzens University of Innsbruck
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.
J Med Chem 47: 6239-47 (2004)
Università
Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.
J Med Chem 47: 6218-29 (2004)
Biogen Idec
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
J Med Chem 47: 6195-206 (2004)
Université
Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.
J Med Chem 47: 6187-94 (2004)
Ghent University
alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.
J Med Chem 47: 6160-73 (2004)
University of Camerino
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.
J Med Chem 47: 6128-36 (2004)
National Institute On Drug Abuse
Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents.
J Med Chem 47: 6124-7 (2004)
Roche Palo Alto
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.
J Med Chem 47: 6117-9 (2004)
Merck Research Laboratories
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.
J Am Chem Soc 126: 15405-11 (2004)
Weizmann Institute of Science
Functional cloning of Bacillus anthracis dihydrofolate reductase and confirmation of natural resistance to trimethoprim.
Antimicrob Agents Chemother 48: 4643-9 (2004)
Oklahoma State University At Stillwater
Pharmacological inhibitors of glycogen synthase kinase 3.
Trends Pharmacol Sci 25: 471-80 (2004)
Rockefeller University
Synthesis and urease enzyme inhibitory effects of some dicoumarols.
J Enzyme Inhib Med Chem 19: 367-71 (2004)
University of Karachi
Conversion of human-selective PPARalpha agonists to human/mouse dual agonists: a molecular modeling analysis.
Bioorg Med Chem Lett 14: 6113-6 (2004)
Eli Lilly
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Bioorg Med Chem Lett 14: 6107-11 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.
Bioorg Med Chem Lett 14: 6095-9 (2004)
Avenida De La Industria
QSAR modelling of HIV-1 reverse transcriptase inhibition by benzoxazinones using a combination of P_VSA and pharmacophore feature descriptors.
Bioorg Med Chem Lett 14: 6089-94 (2004)
S.G.S.I.T.S.
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
Bioorg Med Chem Lett 14: 6083-7 (2004)
University of Newcastle
Novel diarylsulfonylurea derivatives as potent antimitotic agents.
Bioorg Med Chem Lett 14: 6075-8 (2004)
Lg Life Sciences
Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors.
Bioorg Med Chem Lett 14: 6071-4 (2004)
Department of Life Science and National Research Laboratory of Proteolysis
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Bioorg Med Chem Lett 14: 6061-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human beta-tryptase.
Bioorg Med Chem Lett 14: 6053-6 (2004)
Aventis Pharmaceuticals
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 6049-52 (2004)
Nitromed
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
Bioorg Med Chem Lett 14: 6045-8 (2004)
Merck Research Laboratories
Antiviral compounds from traditional Chinese medicines Galla Chinese as inhibitors of HCV NS3 protease.
Bioorg Med Chem Lett 14: 6041-4 (2004)
Peking University
CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.
Bioorg Med Chem Lett 14: 6017-21 (2004)
Cv Therapeutics
Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.
Bioorg Med Chem Lett 14: 6011-6 (2004)
Eli Lilly
Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transporters.
Bioorg Med Chem Lett 14: 6007-10 (2004)
Organix
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
Bioorg Med Chem Lett 14: 6001-6 (2004)
Pennsylvania State University
Alpha-1-C-alkyl-1-deoxynojirimycin derivatives as potent and selective inhibitors of intestinal isomaltase: remarkable effect of the alkyl chain length on glycosidase inhibitory profile.
Bioorg Med Chem Lett 14: 5991-5 (2004)
Orleans University
Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.
Bioorg Med Chem Lett 14: 5975-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.
Bioorg Med Chem Lett 14: 5963-6 (2004)
Dainippon Pharmaceutical
Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.
Bioorg Med Chem Lett 14: 5959-62 (2004)
Dainippon Pharmaceutical
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
J Med Chem 47: 6108-11 (2004)
University of Alberta
Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.
J Med Chem 47: 6070-81 (2004)
University of Florence
Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.
J Med Chem 47: 6034-41 (2004)
Virginia Commonwealth University
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
J Med Chem 47: 6025-33 (2004)
University of Florida
AT2-selective angiotensin II analogues containing tyrosine-functionalized 5,5-bicyclic thiazabicycloalkane dipeptide mimetics.
J Med Chem 47: 6009-19 (2004)
Uppsala University
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.
J Med Chem 47: 5995-6008 (2004)
Uppsala University
Building predictive models for protein tyrosine phosphatase 1B inhibitors based on discriminating structural features by reassembling medicinal chemistry building blocks.
J Med Chem 47: 5984-94 (2004)
Leadscope
5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials.
J Med Chem 47: 5972-83 (2004)
Université
Tetrahydrobiopterin binding to aromatic amino acid hydroxylases. Ligand recognition and specificity.
J Med Chem 47: 5962-71 (2004)
University of Bergen
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
J Med Chem 47: 5953-61 (2004)
Uppsala University
Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.
J Med Chem 47: 5945-52 (2004)
University of Bologna
Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.
J Med Chem 47: 5912-22 (2004)
University of Oxford
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.
J Med Chem 47: 5894-911 (2004)
Bristol-Myers Squibb
Fluorinated phenylcyclopropylamines. 2. Effects of aromatic ring substitution and of absolute configuration on inhibition of microbial tyramine oxidase.
J Med Chem 47: 5860-71 (2004)
Universit£T M£Nster
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.
J Med Chem 47: 5833-6 (2004)
Novartis Institutes For Biomedical Research
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
J Med Chem 47: 5829-32 (2004)
Merck Sharp & Dohme Research Laboratories
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
J Med Chem 47: 5825-8 (2004)
Merck Research Laboratories
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
J Med Chem 47: 5821-4 (2004)
Acenta Discovery
Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides.
Biochemistry 43: 14500-7 (2004)
Glaxosmithkline
Synthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors.
Bioorg Chem 32: 494-503 (2004)
BiomolÉCules Et Cibles Cellulaires Tumorales
Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
J Mol Biol 344: 527-47 (2004)
Celera
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.
Bioorg Med Chem 12: 6171-82 (2004)
Yamanouchi Pharmaceutical
The core structures of roseophilin and the prodigiosin alkaloids define a new class of protein tyrosine phosphatase inhibitors.
Chembiochem 5: 1575-9 (2004)
Max-Planck-Institut FÜR Kohlenforschung
[(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.
J Pharmacol Exp Ther 312: 1114-23 (2005)
Section of Pharmacology
Efficient evaluation of binding free energy using continuum electrostatics solvation.
J Med Chem 47: 5791-7 (2004)
University of ZüRich
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
J Med Chem 47: 5783-90 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.
J Med Chem 47: 5690-9 (2004)
University of Colorado
Structural characterization and pharmacology of a potent (Cys101-Cys119, Cys110-Cys117) bicyclic agouti-related protein (AGRP) melanocortin receptor antagonist.
J Med Chem 47: 5662-73 (2004)
University of Florida
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
J Med Chem 47: 5620-9 (2004)
Budapest University of Technology and Economics
Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor.
J Med Chem 47: 5612-5 (2004)
Trinity College Dublin
A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors.
J Med Chem 47: 5605-7 (2004)
University of Kuopio
NO-sartans: a new class of pharmacodynamic hybrids as cardiovascular drugs.
J Med Chem 47: 5597-600 (2004)
University of Pisa
Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha.
J Med Chem 47: 5593-6 (2004)
X-Ceptor Therapeutics
Factors controlling the complex architecture of native and modified cyclodextrins with dipeptide (Z-Glu-Tyr) studied by microcalorimetry and NMR spectroscopy: critical effects of peripheral bis-trimethylamination and cavity size.
J Am Chem Soc 126: 14224-33 (2004)
Nagoya Institute of Technology
1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.
Bioorg Med Chem Lett 14: 5937-41 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.
Bioorg Med Chem Lett 14: 5925-9 (2004)
Kyoto Pharmaceutical University
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.
Bioorg Med Chem Lett 14: 5907-11 (2004)
Merck Research Laboratories
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.
Bioorg Med Chem Lett 14: 5899-902 (2004)
Schering-Plough Research Institute
Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists.
Bioorg Med Chem Lett 14: 5881-4 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.
Bioorg Med Chem Lett 14: 5867-72 (2004)
Merck Research Laboratories
The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands.
Bioorg Med Chem Lett 14: 5863-6 (2004)
Polish Academy of Sciences
Evaluation of by disubstituted acridone derivatives as telomerase inhibitors: the importance of G-quadruplex binding.
Bioorg Med Chem Lett 14: 5845-9 (2004)
University of London
Synthesis and alpha4beta2 nicotinic affinity of 2-pyrrolidinylmethoxyimines and prolinal oxime ethers.
Bioorg Med Chem Lett 14: 5827-30 (2004)
Università
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.
Bioorg Med Chem Lett 14: 5817-22 (2004)
Merck
Design, synthesis, and evaluation of hexahydrobenz[f]isoquinolines as a novel class of dopamine 3 receptor ligands.
Bioorg Med Chem Lett 14: 5813-6 (2004)
University of Michigan
Synthesis of small molecule CDC25 phosphatases inhibitors.
Bioorg Med Chem Lett 14: 5809-12 (2004)
Institut Henri Beaufour
Inactivation of human S-adenosylhomocysteine hydrolase by covalent labeling of cysteine 195 with thionucleoside derivatives.
Bioorg Med Chem Lett 14: 5803-7 (2004)
Umr 6519
Inactivation of S-adenosylhomocysteine hydrolase with haloethyl and dihalocyclopropyl esters derived from homoadenosine-6'-carboxylic acid.
Bioorg Med Chem Lett 14: 5799-802 (2004)
Umr 6519
Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.
Bioorg Med Chem Lett 14: 5793-7 (2004)
Novartis Institutes For Biomedical Research
Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties.
Bioorg Med Chem Lett 14: 5781-6 (2004)
Joseph Fourier University
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide.
Bioorg Med Chem Lett 14: 5775-80 (2004)
Universita Degli Studi Di Firenze
Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions.
Bioorg Med Chem Lett 14: 5769-73 (2004)
Universita Degli Studi Di Firenze
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet.
Bioorg Med Chem Lett 14: 5763-7 (2004)
Università
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.
Bioorg Med Chem Lett 14: 5751-5 (2004)
Schering-Plough Research Institute
Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors.
Bioorg Med Chem Lett 14: 5739-42 (2004)
Florida A&M University
Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor.
J Enzyme Inhib Med Chem 19: 269-73 (2004)
UniversitÀ Degli Studi Di Firenze
DNA polymerase beta lyase inhibitors from Maytenus putterlickoides.
J Nat Prod 67: 1744-7 (2004)
University of Virginia
Marine sesquiterpenoids that inhibit the lyase activity of DNA polymerase beta.
J Nat Prod 67: 1716-8 (2004)
Virginia Polytechnic Institute and State University
Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea.
J Nat Prod 67: 1681-4 (2004)
Merlion Pharmaceuticals
Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A).
Eur J Pharmacol 503: 25-30 (2004)
Kyoto University Hospital
Dihydrexidine--the first full dopamine D1 receptor agonist.
CNS Drug Rev 10: 230-42 (2004)
Karolinska Institutet
Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance.
Biochemistry 43: 13380-9 (2004)
University of Alabama At Birmingham
Multicopy suppressors for novel antibacterial compounds reveal targets and drug efflux susceptibility.
Chem Biol 11: 1423-30 (2004)
Mcmaster University
Disruption of protein-membrane binding and identification of small-molecule inhibitors of coagulation factor VIII.
Chem Biol 11: 1413-22 (2004)
University of Washington
Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.
Bioorg Med Chem Lett 14: 5709-12 (2004)
Università
Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives.
Bioorg Med Chem Lett 14: 5703-7 (2004)
Università
Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.
Bioorg Med Chem Lett 14: 5693-7 (2004)
Adolor
Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties.
Bioorg Med Chem Lett 14: 5689-92 (2004)
Glaxosmithkline
Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.
Bioorg Med Chem Lett 14: 5685-7 (2004)
Glaxosmithkline
Myxopyronin B analogs as inhibitors of RNA polymerase, synthesis and biological evaluation.
Bioorg Med Chem Lett 14: 5667-72 (2004)
Anadys Pharmaceuticals
Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives.
Bioorg Med Chem Lett 14: 5651-4 (2004)
Cardiff University
Synthesis of 5'-substituted fluoro-neplanocin A analogues: importance of a hydrogen bonding donor at 5'-position for the inhibitory activity of S-adenosylhomocysteine hydrolase.
Bioorg Med Chem Lett 14: 5641-4 (2004)
Pusan National University
Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
Bioorg Med Chem Lett 14: 5635-9 (2004)
Harvard Medical School
Synthesis of 61-bis(1-adamantylcarbamoyl)-1,2-methano[60]fullerene and its antagonistic effect on haloperidol-induced catalepsy in mice.
Bioorg Med Chem Lett 14: 5619-21 (2004)
Kyushu University
QSAR modeling of the MAO inhibitory activity of xanthones derivatives.
Bioorg Med Chem Lett 14: 5611-7 (2004)
Unne
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 14: 5605-9 (2004)
Neurocrine Biosciences
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.
Bioorg Med Chem Lett 14: 5599-603 (2004)
Merck Research Laboratories
Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin.
Bioorg Med Chem Lett 14: 5595-8 (2004)
National Cancer Institute-Frederick
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
Bioorg Med Chem Lett 14: 5591-4 (2004)
Ucb Pharma
Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.
Bioorg Med Chem Lett 14: 5573-7 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.
Bioorg Med Chem Lett 14: 5543-6 (2004)
Abbott Laboratories
Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid.
Bioorg Med Chem Lett 14: 5533-5 (2004)
A.V. Bogatsky Physico-Chemical Institute of The National Academy of Sciences of Ukraine
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.
Bioorg Med Chem Lett 14: 5521-5 (2004)
Pfizer
Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.
Bioorg Med Chem Lett 14: 5513-9 (2004)
Purdue Pharma
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.
Bioorg Med Chem Lett 14: 5509-12 (2004)
Pfizer
A 13C NMR approach to categorizing potential limitations of alpha,beta-unsaturated carbonyl systems in drug-like molecules.
Bioorg Med Chem Lett 14: 5503-7 (2004)
Abbott Bioresearch Center
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.
Bioorg Med Chem Lett 14: 5499-502 (2004)
Wyeth Research
Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists.
Bioorg Med Chem Lett 14: 5493-8 (2004)
Johnson and Johnson Pharmaceutical Research and Development
Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.
Bioorg Med Chem Lett 14: 5489-91 (2004)
Dupont Pharmaceuticals
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.
Bioorg Med Chem Lett 14: 5485-8 (2004)
Merck Research Laboratories
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Bioorg Med Chem Lett 14: 5481-4 (2004)
Merck Research Laboratories
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Bioorg Med Chem Lett 14: 5477-80 (2004)
Merck Research Laboratories
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Bioorg Med Chem Lett 14: 5473-6 (2004)
Merck Research Laboratories
Evaluation of lactam-bridged neurotensin analogues adjusting psi(Pro10) close to the experimentally derived bioactive conformation of NT(8-13).
J Med Chem 47: 5587-90 (2004)
Friedrich-Alexander University
Spectroscopic studies of diketoacids-metal interactions. A probing tool for the pharmacophoric intermetallic distance in the HIV-1 integrase active site.
J Med Chem 47: 5583-6 (2004)
Université
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.
J Med Chem 47: 5555-66 (2004)
Yale University
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
J Med Chem 47: 5535-40 (2004)
University of Ferrara
A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition.
J Med Chem 47: 5492-500 (2004)
University of Kansas
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
J Med Chem 47: 5467-81 (2004)
Pfizer
Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.
J Med Chem 47: 5451-66 (2004)
State University of Groningen
Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups.
J Med Chem 47: 5441-50 (2004)
Leiden University
Influence of the linker in bispyridium compounds on the inhibition of human choline kinase.
J Med Chem 47: 5433-40 (2004)
Universidad De Grenada
A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.
J Med Chem 47: 5418-26 (2004)
Walter Reed Army Institute of Research
Identification and specificity studies of small-molecule ligands for SH3 protein domains.
J Med Chem 47: 5405-17 (2004)
The University of Adelaide
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
J Med Chem 47: 5393-404 (2004)
National Institute of Diabetes and Digestive and Kidney Diseases
Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.
J Med Chem 47: 5381-92 (2004)
Philipps-Universit£T Marburg
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
J Med Chem 47: 5367-80 (2004)
Eli Lilly
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
J Med Chem 47: 5356-66 (2004)
Boehringer Ingelheim Pharmaceuticals
Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition.
J Med Chem 47: 5340-6 (2004)
University of Leicester
HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.
J Med Chem 47: 5336-9 (2004)
Italy. Vinc
Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist.
Br J Pharmacol 143: 649-61 (2004)
Johnson & Johnson Pharmaceutical Research and Development
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.
Cancer Res 64: 7099-109 (2004)
Bayer Pharmaceuticals
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
J Med Chem 47: 5318-29 (2004)
Instituto De Qu£Mica M£Dica (Csic)
Design and synthesis of novel indole beta-diketo acid derivatives as HIV-1 integrase inhibitors.
J Med Chem 47: 5298-310 (2004)
Università
Synthesis and evaluation of nitrofuranylamides as novel antituberculosis agents.
J Med Chem 47: 5276-83 (2004)
University of Tennessee Health Science Center
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.
J Med Chem 47: 5258-64 (2004)
University of Pennsylvania
Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine. Interaction with S-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects.
J Med Chem 47: 5251-7 (2004)
Florida International University
Subtype selective substrates for histone deacetylases.
J Med Chem 47: 5235-43 (2004)
Westf£Lische Wilhelms-Universit£T M£Nster
Carbonic anhydrase inhibitors: the first on-resin screening of a 4-sulfamoylphenylthiourea library.
J Med Chem 47: 5224-9 (2004)
University of Florence
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
J Med Chem 47: 5198-203 (2004)
University of Bologna
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element.
J Med Chem 47: 5167-82 (2004)
Daiichi Pharmaceutical
Effects of altering the electronics of 2-methoxyestradiol on cell proliferation, on cytotoxicity in human cancer cell cultures, and on tubulin polymerization.
J Med Chem 47: 5126-39 (2004)
Purdue University
Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine transporters.
J Med Chem 47: 5101-13 (2004)
Wayne State University
Identification and characterization of small molecule inhibitors of the calcium-dependent S100B-p53 tumor suppressor interaction.
J Med Chem 47: 5085-93 (2004)
University of Maryland
Soft docking and multiple receptor conformations in virtual screening.
J Med Chem 47: 5076-84 (2004)
University of California San Francisco
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
J Med Chem 47: 5069-75 (2004)
University of Bath
Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.
J Med Chem 47: 5057-68 (2004)
Glaxosmithkline
Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.
J Med Chem 47: 5049-56 (2004)
Glaxosmithkline
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
J Med Chem 47: 5021-40 (2004)
Wyeth Research
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
J Med Chem 47: 5009-20 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.
J Med Chem 47: 4998-5008 (2004)
Università
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
J Med Chem 47: 4985-8 (2004)
The Pennsylvania State University
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 5445-8 (2004)
Glaxosmithkline
Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions.
Bioorg Med Chem Lett 14: 5435-9 (2004)
Universita Degli Studi Di Firenze
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
Bioorg Med Chem Lett 14: 5427-33 (2004)
Universita Degli Studi Di Firenze
Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives.
Bioorg Med Chem Lett 14: 5413-6 (2004)
Deltagen Research Laboratories
Small molecule inhibitors of the CCR2b receptor. Part 1: Discovery and optimization of homopiperazine derivatives.
Bioorg Med Chem Lett 14: 5407-11 (2004)
Institute For Bio-Medical Research
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.
Bioorg Med Chem Lett 14: 5389-94 (2004)
Astrazeneca
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.
Bioorg Med Chem Lett 14: 5383-7 (2004)
Astrazeneca
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
Bioorg Med Chem Lett 14: 5377-81 (2004)
Research Triangle Institute
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.
Bioorg Med Chem Lett 14: 5371-6 (2004)
Abbott Laboratories
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Bioorg Med Chem Lett 14: 5367-70 (2004)
Abbott Laboratories
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.
Bioorg Med Chem Lett 14: 5343-6 (2004)
Crest Research Project
Three new compounds from the plant Lippia alva as inhibitors of chemokine receptor 5 (CCR5).
Bioorg Med Chem Lett 14: 5339-42 (2004)
Schering-Plough Research Institute
HCV NS5B polymerase-bound conformation of a soluble sulfonamide inhibitor by 2D transferred NOESY.
Bioorg Med Chem Lett 14: 5333-7 (2004)
Virochem Pharma
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.
Bioorg Med Chem Lett 14: 5329-32 (2004)
Merck Research Laboratories
Substrate analogs for the investigation of deoxyxylulose 5-phosphate reductoisomerase inhibition: synthesis and evaluation.
Bioorg Med Chem Lett 14: 5309-12 (2004)
Oregon State University
More potent linear peptide inhibitors of mammalian ribonucleotide reductase.
Bioorg Med Chem Lett 14: 5301-4 (2004)
University of Pennsylvania
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.
Bioorg Med Chem Lett 14: 5295-300 (2004)
Maxim Pharmaceuticals
Synthesis and structure-activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands.
Bioorg Med Chem Lett 14: 5285-8 (2004)
The University of Michigan Medical School
Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity.
Bioorg Med Chem Lett 14: 5281-4 (2004)
Wyeth Research
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Bioorg Med Chem Lett 14: 5275-9 (2004)
Purdue Pharma
5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.
Bioorg Med Chem Lett 14: 5269-73 (2004)
Bristol-Myers Squibb
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Bioorg Med Chem Lett 14: 5263-7 (2004)
Bristol-Myers Squibb
Synthesis and enzymatic evaluation of xanthine oxidase-activated prodrugs based on inhibitors of thymidine phosphorylase.
Bioorg Med Chem Lett 14: 5247-50 (2004)
University of Manchester
Design and synthesis of indole and tetrahydroisoquinoline hydantoin derivatives as human chymase inhibitors.
J Enzyme Inhib Med Chem 19: 137-43 (2004)
UniversitÉ
Biscoumarin derivatives from Edgeworthia gardneri that inhibit the lyase activity of DNA polymerase beta.
J Nat Prod 67: 1608-10 (2004)
University of Virginia
BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.
J Nat Prod 67: 1528-31 (2004)
Boehringer Ingelheim Pharma Gmbh And
Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A.
Biopharm Drug Dispos 25: 283-9 (2004)
Tufts University School of Medicine
Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.
J Pharmacol Exp Ther 312: 220-30 (2005)
Temple University
Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
Bioorg Med Chem Lett 14: 5227-32 (2004)
Johnson & Johnson Pharmaceutical Research and Development
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
Bioorg Med Chem Lett 14: 5223-6 (2004)
Abbott Laboratories
Facile incorporation of urea pseudopeptides into protease substrate analogue inhibitors.
Bioorg Med Chem Lett 14: 5219-22 (2004)
Purdue University
Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Bioorg Med Chem Lett 14: 5215-8 (2004)
Upres Ea 1085 BiomoléCules Et Cibles Cellulaires Tumorales
Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
Bioorg Med Chem Lett 14: 5205-9 (2004)
University of Mainz
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
Bioorg Med Chem Lett 14: 5199-203 (2004)
University of California San Francisco
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
Bioorg Med Chem Lett 14: 5193-8 (2004)
Daiichi Pharmaceutical
Synthesis of 5a-carba-hexopyranoses and hexopyranosylamines, as well as 5a,5a'-dicarbadisaccharides, from 3,8-dioxatricyclo[4.2.1.0(2,4)]nonan-9-ol: glycosidase inhibitory activity of N-substituted 5a-carba-beta-gluco- and beta-galactopyranosylamines, and derivatives thereof.
Bioorg Med Chem Lett 14: 5183-8 (2004)
Keio University
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.
Bioorg Med Chem Lett 14: 5171-4 (2004)
Central Pharmaceutical Research Institute
N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.
Bioorg Med Chem Lett 14: 5157-60 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent and selective proline derived dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 5151-5 (2004)
Merck
Glycosylated dihydrochalcones as potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitors.
Bioorg Med Chem Lett 14: 5121-5 (2004)
Johnson & Johnson Pharmaceutical Research and Development
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).
Bioorg Med Chem Lett 14: 5113-6 (2004)
University of Southern California
Benzothiophene and naphthalene derived constrained SERMs.
Bioorg Med Chem Lett 14: 5103-6 (2004)
Eli Lilly
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
Bioorg Med Chem Lett 14: 5095-8 (2004)
Abbott Laboratories
Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid.
Bioorg Med Chem Lett 14: 5085-8 (2004)
Mrl Rome
Development of a polyvalent assay system for lead identification.
Bioorg Med Chem Lett 14: 5081-3 (2004)
Wyeth Research
4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists.
Bioorg Med Chem Lett 14: 5075-80 (2004)
7Tm Pharma
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
Bioorg Med Chem Lett 14: 5067-70 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Bioorg Med Chem Lett 14: 5057-62 (2004)
Abbott Laboratories
1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.
Bioorg Med Chem Lett 14: 5045-50 (2004)
Purdue Pharma
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.
Biochemistry 43: 12141-51 (2004)
University of Florida College of Medicine
Molecular design of cholesterols as inhibitors of DNA polymerase alpha.
J Med Chem 47: 4971-4 (2004)
Frontier Research Center For Genome & Drug Discovery
A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.
J Med Chem 47: 4950-7 (2004)
Novartis Institutes For Biomedical Research and Novartis Pharma Development
Macrocyclic inhibitors for peptide deformylase: a structure-activity relationship study of the ring size.
J Med Chem 47: 4941-9 (2004)
The Ohio State University
Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal.
J Med Chem 47: 4881-90 (2004)
Università
Novel cyclooxygenase-1 inhibitors discovered using affinity fingerprints.
J Med Chem 47: 4875-80 (2004)
Telik
Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).
J Med Chem 47: 4858-64 (2004)
National Cancer Institute-Frederick
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
J Med Chem 47: 4829-37 (2004)
Merck Research Laboratories
Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.
J Med Chem 47: 4799-801 (2004)
Johnson & Johnson Pharmaceutical Research and Development
Bisubstrate inhibitors of the enzyme catechol O-methyltransferase (COMT): efficient inhibition despite the lack of a nitro group.
Chembiochem 5: 1270-4 (2004)
Laboratorium FÜR Organische Chemie
Inhibition of Golgi mannosidase II with mannostatin A analogues: synthesis, biological evaluation, and structure-activity relationship studies.
Chembiochem 5: 1220-7 (2004)
University of Georgia
Transport characteristics of fexofenadine in the Caco-2 cell model.
Pharm Res 21: 1398-404 (2004)
Uppsala University
Non-peptide oxytocin agonists.
Bioorg Med Chem Lett 14: 4585-9 (2004)
Ferring Research
SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.
Bioorg Med Chem Lett 14: 4575-9 (2004)
Merck Research Laboratories
Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors.
Bioorg Med Chem Lett 14: 4569-73 (2004)
Virginia Commonwealth University
Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the methanoarchaeon Methanobacterium thermoautotrophicum (Cab) with anions.
Bioorg Med Chem Lett 14: 4563-7 (2004)
Universita Degli Studi Di Firenze
Discovery of new chemical leads for prostaglandin D2 receptor antagonists.
Bioorg Med Chem Lett 14: 4557-62 (2004)
Minase Research Institute
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands.
Bioorg Med Chem Lett 14: 4553-5 (2004)
3-Dimensional Pharmaceuticals
Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives.
Bioorg Med Chem Lett 14: 4549-51 (2004)
Guilford Pharmaceuticals
Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.
Bioorg Med Chem Lett 14: 4539-44 (2004)
Merck Research Laboratory
AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey.
Bioorg Med Chem Lett 14: 4525-8 (2004)
Alcon Research
Substituted 6-phenyl-pyridin-2-ylamines: selective and potent inhibitors of neuronal nitric oxide synthase.
Bioorg Med Chem Lett 14: 4511-4 (2004)
Pfizer
Isoindolinone ureas: a novel class of KDR kinase inhibitors.
Bioorg Med Chem Lett 14: 4505-9 (2004)
Abbott Laboratories
The purine transferase from Trypanosoma cruzi as a potential target for bisphosphonate-based chemotherapeutic compounds.
Bioorg Med Chem Lett 14: 4501-4 (2004)
Universidad De Buenos Aires
Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity.
Bioorg Med Chem Lett 14: 4467-70 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.
Bioorg Med Chem Lett 14: 4461-5 (2004)
Korea Research Institute of Chemical Technology
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.
Bioorg Med Chem Lett 14: 4453-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.
Bioorg Med Chem Lett 14: 4449-52 (2004)
Biovitrum
Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.
Bioorg Med Chem Lett 14: 4445-8 (2004)
Biovitrum
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 14: 4417-23 (2004)
Neurocrine Biosciences
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.
Bioorg Med Chem Lett 14: 4411-5 (2004)
Merck Research Laboratories
Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog.
Bioorg Med Chem Lett 14: 4395-8 (2004)
Conjuchem
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.
Bioorg Med Chem Lett 14: 4379-82 (2004)
Brigham & Women'S Hospital
Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.
Bioorg Med Chem Lett 14: 4375-8 (2004)
Glaxosmithkline
Heterologous expression of human {alpha}6{beta}4{beta}3{alpha}5 nicotinic acetylcholine receptors: binding properties consistent with their natural expression require quaternary subunit assembly including the {alpha}5 subunit.
J Pharmacol Exp Ther 312: 619-26 (2005)
Targacept
Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential.
J Pharmacol Exp Ther 312: 561-70 (2005)
University of Piemonte Orientale
Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening.
J Biol Chem 279: 50555-65 (2004)
The Scripps Research Institute
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Bioorg Med Chem Lett 14: 5007-11 (2004)
Eli Lilly
Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase.
Bioorg Med Chem Lett 14: 4999-5002 (2004)
Novartis Institutes For Biomedical Research Gdc
Synthesis of acyloxymethyl ester prodrugs of the transferable protein farnesyl transferase substrate farnesyl methylenediphosphonate.
Bioorg Med Chem Lett 14: 4979-82 (2004)
University of Kentucky
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.
Bioorg Med Chem Lett 14: 4967-73 (2004)
Neurocrine Biosciences
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.
Bioorg Med Chem Lett 14: 4945-8 (2004)
Procter and Gamble Pharmaceuticals
Synthesis and evaluation of novel oxazoline MMP inhibitors.
Bioorg Med Chem Lett 14: 4935-9 (2004)
North Dakota State University
7-Substituted 2-phenyl-benzofurans as ER beta selective ligands.
Bioorg Med Chem Lett 14: 4925-9 (2004)
Wyeth Research
The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.
Bioorg Med Chem Lett 14: 4915-8 (2004)
Athersys
A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 4911-4 (2004)
University of Alberta
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
Bioorg Med Chem Lett 14: 4903-6 (2004)
University of Virginia
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.
Bioorg Med Chem Lett 14: 4897-902 (2004)
Glaxosmithkline
Discovery of orally active prostaglandin D2 receptor antagonists.
Bioorg Med Chem Lett 14: 4891-5 (2004)
Minase Research Institute
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.
Bioorg Med Chem Lett 14: 4883-6 (2004)
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
Bioorg Med Chem Lett 14: 4879-82 (2004)
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
Bioorg Med Chem Lett 14: 4873-7 (2004)
Abbott Laboratories
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor.
Bioorg Med Chem Lett 14: 4867-72 (2004)
In Vivo Sciences Millennium Pharmaceuticals
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Bioorg Med Chem Lett 14: 4861-6 (2004)
Merck Research Laboratories
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.
Bioorg Med Chem Lett 14: 4851-4 (2004)
Ewha Womans University
N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.
Bioorg Med Chem Lett 14: 4847-50 (2004)
Nps Pharmaceuticals
Modeling the binding affinities of beta-secretase inhibitors: application to subsite specificity.
Bioorg Med Chem Lett 14: 4843-6 (2004)
Johnson & Johnson Pharmaceutical Research and Development
End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists.
Bioorg Med Chem Lett 14: 4839-42 (2004)
University of Cincinnati
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
Bioorg Med Chem Lett 14: 4835-8 (2004)
Biogen Idec
Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
Bioorg Med Chem Lett 14: 4831-4 (2004)
Biogen Idec
Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.
Bioorg Med Chem Lett 14: 4819-23 (2004)
Aventis Pharmaceuticals
Inhibition of the strand transfer step of HIV-1 integrase by non-natural dinucleotides.
Bioorg Med Chem Lett 14: 4815-7 (2004)
University of Georgia
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.
J Med Chem 47: 4787-98 (2004)
Neurocrine Biosciences
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).
J Med Chem 47: 4774-86 (2004)
Wyeth Research
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.
J Med Chem 47: 4766-73 (2004)
Cv Therapeutics
Dipeptidomimetic ketomethylene isosteres as pro-moieties for drug transport via the human intestinal di-/tripeptide transporter hPEPT1: design, synthesis, stability, and biological investigations.
J Med Chem 47: 4755-65 (2004)
University of Tromsø
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.
J Med Chem 47: 4741-54 (2004)
Pharmaceutical Research Institute
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.
J Med Chem 47: 4716-30 (2004)
Glaxosmithkline
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
J Med Chem 47: 4684-92 (2004)
Merck
Indolebutylamines as selective 5-HT(1A) agonists.
J Med Chem 47: 4677-83 (2004)
Merck
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
J Med Chem 47: 4645-8 (2004)
TBA
Potent and orally bioavailable non-peptide antagonists at the human bradykinin B(1) receptor based on a 2-alkylamino-5-sulfamoylbenzamide core.
J Med Chem 47: 4642-4 (2004)
TBA
Virulence regulation and quorum sensing in staphylococcal infections: competitive AgrC antagonists as quorum sensing inhibitors.
J Med Chem 47: 4633-41 (2004)
University of Nottingham
Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea.
J Nat Prod 67: 1291-4 (2004)
Griffith University
An analysis of phakellin and oroidin structures stimulated by further study of an Agelas sponge.
J Nat Prod 67: 1256-61 (2004)
University of California
Intrinsic and acquired forms of resistance against the anticancer ruthenium compound KP1019 [indazolium trans-[tetrachlorobis(1H-indazole)ruthenate (III)] (FFC14A).
J Pharmacol Exp Ther 312: 281-9 (2004)
Institute of Cancer Research
Design and synthesis of substituted N-methylbenzamide analogues derived from SR 48,968 as neurokinin-2 receptor antagonists.
Bioorg Med Chem Lett 14: 4779-82 (2004)
St. John'S University
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
Bioorg Med Chem Lett 14: 4771-7 (2004)
China Pharmaceutical University
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 4763-6 (2004)
Merck
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 4759-62 (2004)
Merck
Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 4741-5 (2004)
Roche Palo Alto
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Bioorg Med Chem Lett 14: 4731-3 (2004)
Clinical Research Institute of Montreal
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.
Bioorg Med Chem Lett 14: 4727-30 (2004)
Pfizer
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
Bioorg Med Chem Lett 14: 4705-10 (2004)
Novartis Horsham Research Centre
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.
Bioorg Med Chem Lett 14: 4697-9 (2004)
Virginia Commonwealth University
Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA:cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size.
Bioorg Med Chem Lett 14: 4677-81 (2004)
National Research Laboratory of Lipid Metabolism and Atherosclerosis
Exploring QSAR with E-state index: selectivity requirements for COX-2 versus COX-1 binding of terphenyl methyl sulfones and sulfonamides.
Bioorg Med Chem Lett 14: 4665-70 (2004)
Jadavpur University
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.
Bioorg Med Chem Lett 14: 4659-63 (2004)
Universit£T Regensburg
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
Bioorg Med Chem Lett 14: 4651-4 (2004)
Merck Research Laboratories
Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett 14: 4639-42 (2004)
Shanghai Institute of Materia Medica
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.
Bioorg Med Chem Lett 14: 4627-31 (2004)
Pfizer
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.
Bioorg Med Chem Lett 14: 4623-6 (2004)
Pfizer
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Bioorg Med Chem Lett 14: 4607-13 (2004)
Pfizer
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Bioorg Med Chem Lett 14: 4603-6 (2004)
Abbott Laboratories
Selective Itk inhibitors block T-cell activation and murine lung inflammation.
NA
Bristol-Myers Squibb Pharmaceutical Research Institute
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
Naunyn Schmiedebergs Arch Pharmacol 370: 114-23 (2004)
Vernalis Research
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of"THIQ".
J Med Chem 47: 4613-26 (2004)
Uppsala University
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist.
J Med Chem 47: 4588-94 (2004)
Research Triangle Institute
Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.
J Med Chem 47: 4570-87 (2004)
Taisho Pharmaceutical
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.
J Med Chem 47: 4559-69 (2004)
University of Perugia
High-resolution structures of human aldose reductase holoenzyme in complex with stereoisomers of the potent inhibitor Fidarestat: stereospecific interaction between the enzyme and a cyclic imide type inhibitor.
J Med Chem 47: 4530-7 (2004)
Monash University (Parkville Campus)
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
J Med Chem 47: 4517-29 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
J Med Chem 47: 4494-506 (2004)
Glaxosmithkline
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity toward the alpha2-adrenoceptor.
J Med Chem 47: 4483-93 (2004)
University of Kansas
Modulation of binding strength in several classes of active site inhibitors of acetylcholinesterase studied by comparative binding energy analysis.
J Med Chem 47: 4471-82 (2004)
Universitat De Barcelona
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
J Med Chem 47: 4417-26 (2004)
Abbott Laboratories
Molecular recognition in purinergic receptors. 2. Diastereoselectivity of the h-P2Y1-receptor.
J Med Chem 47: 4405-16 (2004)
Bar-Ilan University
Determinants of retinoid X receptor transcriptional antagonism.
J Med Chem 47: 4360-72 (2004)
Institute
Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions.
Cancer Res 64: 5804-11 (2004)
The Netherlands Cancer Institute
In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892.
Br J Pharmacol 143: 81-90 (2004)
Abbott Laboratories
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.
J Med Chem 47: 4300-15 (2004)
Umr Cnrs/Ulp 7081
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
J Med Chem 47: 4291-9 (2004)
Biogen Idec
Identification of structurally diverse growth hormone secretagogue agonists by virtual screening and structure-activity relationship analysis of 2-formylaminoacetamide derivatives.
J Med Chem 47: 4286-90 (2004)
Institute For Life Science Research
2-(1-adamantyl)-4-(thio)chromenone-6-carboxylic acids: potent reversible inhibitors of human steroid sulfatase.
J Med Chem 47: 4268-76 (2004)
Novartis Institute For Biomedical Research Vienna
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach.
J Med Chem 47: 4258-67 (2004)
Università
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
J Med Chem 47: 4247-57 (2004)
National Health Research Institutes
Design, synthesis, and biological evaluation of new cyclic disulfide decapeptides that inhibit the binding of AP-1 to DNA.
J Med Chem 47: 4239-46 (2004)
Toyama Chemical
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
J Med Chem 47: 4213-30 (2004)
Abbott Laboratories
Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.
J Med Chem 47: 4202-12 (2004)
University of Milan
A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.
J Med Chem 47: 4163-5 (2004)
Virginia Commonwealth University
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
J Med Chem 47: 4155-8 (2004)
Friedrich-Schiller-UniversitäT Jena
Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.
J Med Chem 47: 4151-4 (2004)
Fujisawa Pharmaceutical
Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site.
J Med Chem 47: 4147-50 (2004)
University of Michigan
Prospects for inhibitors of protein tyrosine phosphatase 1B as antidiabetic drugs.
J Med Chem 47: 4142-6 (2004)
Serono Pharmaceutical Research Institute
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
J Med Chem 47: 4135-41 (2004)
Merck Research Laboratories
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
J Med Chem 47: 4118-27 (2004)
Glaxosmithkline
New crinine-type alkaloids with inhibitory effect on induction of inducible nitric oxide synthase from Crinum yemense.
J Nat Prod 67: 1119-24 (2004)
Mansoura University
Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.
J Nat Prod 67: 1079-83 (2004)
Toyama Medical and Pharmaceutical University
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.
J Med Chem 47: 4083-8 (2004)
Neurocrine Biosciences
Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.
J Med Chem 47: 4066-71 (2004)
University of Cagliary
Probing the activity differences of simple and complex brominated aryl compounds against 15-soybean, 15-human, and 12-human lipoxygenase.
J Med Chem 47: 4060-5 (2004)
University of California
Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.
J Med Chem 47: 4054-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.
J Med Chem 47: 4041-53 (2004)
Iiqab (Csic)
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
J Med Chem 47: 4032-40 (2004)
Ohio State University
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
J Med Chem 47: 3972-90 (2004)
University of Alberta
A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.
J Med Chem 47: 3962-71 (2004)
Argenta Discovery
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
J Med Chem 47: 3934-7 (2004)
Eli Lilly
Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase.
J Med Chem 47: 3931-3 (2004)
Harvard Medical School
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.
J Med Chem 47: 3927-30 (2004)
Uppsala University
Design, synthesis, and evaluation of sugar amino acid based inhibitors of protein prenyl transferases PFT and PGGT-1.
J Med Chem 47: 3920-3 (2004)
Leiden University
Synthesis, biophysical and biological evaluation of 3,6-bis-amidoacridines with extended 9-anilino substituents as potent G-quadruplex-binding telomerase inhibitors.
Bioorg Med Chem Lett 14: 4347-51 (2004)
University of London School of Pharmacy
Design and synthesis of novel Cdc25A-inhibitors having phosphate group as a hydrophilic residue.
Bioorg Med Chem Lett 14: 4339-42 (2004)
The University of Tokyo
P4 cap modified tetrapeptidyl alpha-ketoamides as potent HCV NS3 protease inhibitors.
Bioorg Med Chem Lett 14: 4333-8 (2004)
Eli Lilly
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.
Bioorg Med Chem Lett 14: 4319-21 (2004)
Michigan State University
Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8 (IL-8) receptor antagonists.
Bioorg Med Chem Lett 14: 4307-11 (2004)
Johnson and Johnson Pharmaceutical Research and Development
A unidirectional crosslinking strategy for HIV-1 protease dimerization inhibitors.
Bioorg Med Chem Lett 14: 4297-300 (2004)
Purdue University
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.
Bioorg Med Chem Lett 14: 4291-5 (2004)
Merck Frosst Centre For Therapeutic Research
Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.
Bioorg Med Chem Lett 14: 4281-6 (2004)
Central Pharmaceutical Research Institute
Acyl-CoA: cholesterol acyltransferase inhibitory activities of fatty acid amides isolated from Mylabris phalerate Pallas.
Bioorg Med Chem Lett 14: 4277-80 (2004)
Korea Research Institute of Bioscience and Biotechnology
Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.
Bioorg Med Chem Lett 14: 4263-6 (2004)
Institute For Biological Research
Diaminopyrimidine and diaminopyridine 5-HT7 ligands.
Bioorg Med Chem Lett 14: 4249-52 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminotriazine 5-HT7 antagonists.
Bioorg Med Chem Lett 14: 4245-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.
Bioorg Med Chem Lett 14: 4237-40 (2004)
Cyclacel
Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SKCa channels in sympathetic neurons.
Bioorg Med Chem Lett 14: 4231-5 (2004)
Aristotelian University of Thessaloniki
Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.
Bioorg Med Chem Lett 14: 4225-9 (2004)
Johnson and Johnson Pharmaceutical Research and Development
Identification of [(naphthalene-1-carbonyl)-amino]-acetic acid derivatives as nonnucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase.
Bioorg Med Chem Lett 14: 4221-4 (2004)
Wyeth Research
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
Bioorg Med Chem Lett 14: 4217-20 (2004)
University of Michigan
Copper dipicolinates as peptidomimetic ligands for the Src SH2 domain.
Bioorg Med Chem Lett 14: 4203-6 (2004)
Darmstadt Technical University
Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
Bioorg Med Chem Lett 14: 4197-201 (2004)
Aventis Pharma Deutschland
Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.
Bioorg Med Chem Lett 14: 4191-5 (2004)
Aventis Pharma Deutschland
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
Bioorg Med Chem Lett 14: 4179-83 (2004)
Abbott Laboratories
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
Bioorg Med Chem Lett 14: 4173-8 (2004)
Abbott Laboratories
Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.
Bioorg Med Chem Lett 14: 4169-72 (2004)
Abbott Laboratories
Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors.
Bioorg Med Chem Lett 14: 4165-8 (2004)
Abbott Laboratories
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Bioorg Med Chem Lett 14: 4161-4 (2004)
Merck Research Laboratories
Benzodiazepine inhibitors of the MMPs and TACE. Part 2.
Bioorg Med Chem Lett 14: 4147-51 (2004)
Wyeth Research
Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor.
J Pharmacol Exp Ther 311: 537-46 (2004)
Neurocrine Biosciences
Fluorescence polarization assay and inhibitor design for MDM2/p53 interaction.
Anal Biochem 331: 138-46 (2004)
Schering-Plough Research Institute
Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.
Biochem Biophys Res Commun 320: 672-9 (2004)
Chosun University
Synthesis and biological evaluation of 2-phenylpyran-4-ones: a new class of orally active cyclooxygenase-2 inhibitors.
J Med Chem 47: 3874-86 (2004)
RhôNe-Poulenc Rorer
Synthesis and biological evaluation of a new class of geldanamycin derivatives as potent inhibitors of Hsp90.
J Med Chem 47: 3865-73 (2004)
Conforma Therapeutics
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
J Med Chem 47: 3853-64 (2004)
Abbott Laboratories
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
J Med Chem 47: 3823-42 (2004)
Wyeth Research
Novel azapeptide inhibitors of hepatitis C virus serine protease.
J Med Chem 47: 3788-99 (2004)
Boehringer Ingelheim (Canada)
Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors.
J Med Chem 47: 3730-43 (2004)
Fujisawa Pharmaceutical
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.
J Med Chem 47: 3710-22 (2004)
University of Newcastle
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
J Med Chem 47: 3707-9 (2004)
University of Leiden
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.
Bioorg Med Chem Lett 14: 4099-102 (2004)
Argenta Discovery
Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect.
Bioorg Med Chem Lett 14: 4083-5 (2004)
Johnson and Johnson Pharmaceutical
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.
Bioorg Med Chem Lett 14: 4075-8 (2004)
Abbott Laboratories
A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist.
Bioorg Med Chem Lett 14: 4069-74 (2004)
University of Virginia
The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors.
Bioorg Med Chem Lett 14: 4027-30 (2004)
H. Lundbeck
Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents.
Bioorg Med Chem Lett 14: 4019-22 (2004)
Kyoto 619-0216
Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 2: Improvement of in vitro activity.
Bioorg Med Chem Lett 14: 4013-7 (2004)
Kyoto 619-0216
Quantitative structure-activity relationship analysis of a series of 2,3-diaryl benzopyran analogues as novel selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 4005-11 (2004)
Devi Ahilya Vishwavidyalaya
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Bioorg Med Chem Lett 14: 3993-6 (2004)
Merck Research Laboratories
Aza-boronic acids as non-beta-lactam inhibitors of AmpC-beta-lactamase.
Bioorg Med Chem Lett 14: 3979-83 (2004)
Università
Rhodanine-3-acetic acid derivatives as inhibitors of fungal protein mannosyl transferase 1 (PMT1).
Bioorg Med Chem Lett 14: 3975-8 (2004)
Celltech R&D
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-disubstituted ureas.
Bioorg Med Chem Lett 14: 3971-4 (2004)
Procyon Biopharma
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.
Bioorg Med Chem Lett 14: 3967-70 (2004)
Schering-Plough Research Institute
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.
Bioorg Med Chem Lett 14: 3963-6 (2004)
University of Erlangen-Nuremberg
Solution phase parallel synthesis and evaluation of MAPK inhibitory activities of close structural analogues of a Ras pathway modulator.
Bioorg Med Chem Lett 14: 3957-62 (2004)
Morphochem
Oxamides as novel NR2B selective NMDA receptor antagonists.
Bioorg Med Chem Lett 14: 3953-6 (2004)
Gedeon Richter
Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.
Bioorg Med Chem Lett 14: 3943-7 (2004)
Neurocrine Biosciences
Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues.
Bioorg Med Chem Lett 14: 3937-41 (2004)
Glaxosmithkline
Cinnamic acid esters as potent inhibitors of fungal 17beta-hydroxysteroid dehydrogenase--a model enzyme of the short-chain dehydrogenase/reductase superfamily.
Bioorg Med Chem Lett 14: 3933-6 (2004)
University of Ljubljana
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.
Bioorg Med Chem Lett 14: 3925-8 (2004)
Eli Lilly
4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors.
Bioorg Med Chem Lett 14: 3907-11 (2004)
Tsukuba Research Laboratories
Privileged scaffolds for blocking protein-protein interactions: 1,4-disubstituted naphthalene antagonists of transcription factor complex HOX-PBX/DNA.
Bioorg Med Chem Lett 14: 3875-9 (2004)
The State University of New York
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.
Bioorg Med Chem Lett 14: 3869-73 (2004)
Neurocrine Bioscience
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.
Bioorg Med Chem Lett 14: 3865-8 (2004)
Merck Research Laboratories
Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.
Bioorg Med Chem Lett 14: 3861-4 (2004)
Merck Research Laboratories
Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.
Chem Biol 11: 775-85 (2004)
Vernalis (R&D)
Isolation and structure of antagonists of chemokine receptor (CCR5).
J Nat Prod 67: 1036-8 (2004)
Merck Research Laboratories
First synthesis and determination of the absolute configuration of sulphostin, a novel inhibitor of dipeptidyl peptidase IV.
J Nat Prod 67: 999-1004 (2004)
Microbial Chemistry Research Center
New neolignans that inhibit DNA polymerase beta lyase.
J Nat Prod 67: 964-7 (2004)
Virginia Polytechnic Institute and State University
Synthesis and antibacterial activity of a novel series of potent DNA gyrase inhibitors. Pyrazole derivatives.
J Med Chem 47: 3693-6 (2004)
Dainippon Pharmaceutical
Design, synthesis, and biological evaluation of 2,4-diamino-5-methyl-6-substituted-pyrrolo[2,3-d]pyrimidines as dihydrofolate reductase inhibitors.
J Med Chem 47: 3689-92 (2004)
Duquesne University
Mechanism of inactivation of beta-lactamases by novel 6-methylidene penems elucidated using electrospray ionization mass spectrometry.
J Med Chem 47: 3674-88 (2004)
Wyeth Research
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.
J Med Chem 47: 3642-57 (2004)
Merck Sharp and Dohme Research Laboratories
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
J Med Chem 47: 3591-9 (2004)
Kobe Gakuin University
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.
J Med Chem 47: 3580-90 (2004)
Universita Degli Studi Di Firenze
Computer-assisted design of selective imidazole inhibitors for cytochrome p450 enzymes.
J Med Chem 47: 3572-9 (2004)
University of California
Synthesis, biological activity, and three-dimensional quantitative structure-activity relationship model for a series of benzo[c]quinolizin-3-ones, nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
J Med Chem 47: 3546-60 (2004)
University of Florence
Identification, synthesis, and characterization of new glycogen phosphorylase inhibitors binding to the allosteric AMP site.
J Med Chem 47: 3537-45 (2004)
Novo Nordisk
Identification of non-phosphate-containing small molecular weight inhibitors of the tyrosine kinase p56 Lck SH2 domain via in silico screening against the pY + 3 binding site.
J Med Chem 47: 3502-11 (2004)
University of Maryland
Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization.
J Med Chem 47: 3491-4 (2004)
Wyeth Research
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.
J Med Chem 47: 3483-6 (2004)
Neurocrine Biosciences
Fragment-based drug discovery.
J Med Chem 47: 3463-82 (2004)
Sunesis Pharmaceuticals
Novel dual inhibitors of calpain and lipid peroxidation.
Bioorg Med Chem Lett 14: 3825-8 (2004)
Institut Henri Beaufour
Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Bioorg Med Chem Lett 14: 3799-802 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents.
Bioorg Med Chem Lett 14: 3793-7 (2004)
Cv Therapeutics
(+)-3-[2-(Benzo[b]thiophen-2-yl)-2-oxoethyl]-1-azabicyclo[2.2.2]octane as potent agonists for the alpha7 nicotinic acetylcholine receptor.
Bioorg Med Chem Lett 14: 3781-4 (2004)
Mitsubishi Pharma
Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.
Bioorg Med Chem Lett 14: 3775-9 (2004)
Otsuka Pharmaceutical Factory
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.
Bioorg Med Chem Lett 14: 3763-9 (2004)
Merck
Carbonic anhydrase inhibitors. Inhibition of cytosolic isozyme XIII with aromatic and heterocyclic sulfonamides: a novel target for the drug design.
Bioorg Med Chem Lett 14: 3757-62 (2004)
University of Tampere
Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.
Bioorg Med Chem Lett 14: 3753-5 (2004)
Merck Research Laboratories
Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains.
Bioorg Med Chem Lett 14: 3747-51 (2004)
Merck Research Laboratories
Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the alpha3beta4* nicotinic acetylcholine receptors through modifications to the ester.
Bioorg Med Chem Lett 14: 3739-42 (2004)
Ohio University
Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.
Bioorg Med Chem Lett 14: 3727-31 (2004)
3-Dimensional Pharmaceuticals
Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).
Bioorg Med Chem Lett 14: 3721-5 (2004)
Millennium Pharmaceuticals
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.
Bioorg Med Chem Lett 14: 3715-20 (2004)
Aventis Pharma Deutschland
Inhibition of monoamine oxidases by coumarin-3-acyl derivatives: biological activity and computational study.
Bioorg Med Chem Lett 14: 3697-703 (2004)
Sapienza University of Rome
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.
Bioorg Med Chem Lett 14: 3669-73 (2004)
Neurocrine Biosciences
Antimitotic activity of glaupalol-related coumarins from Glaucidium palmatum.
Bioorg Med Chem Lett 14: 3665-8 (2004)
Hokkaido University
Structural variations in keto-glutamines for improved inhibition against hepatitis A virus 3C proteinase.
Bioorg Med Chem Lett 14: 3655-8 (2004)
University of Alberta
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Bioorg Med Chem Lett 14: 3651-4 (2004)
Virginia Commonwealth University
Discovery of small molecule antagonists of TRPV1.
Bioorg Med Chem Lett 14: 3631-4 (2004)
Gsk
Synthesis of hydroxy derivatives of highly potent non-steroidal CYP 17 inhibitors as potential metabolites and evaluation of their activity by a non cellular assay using recombinant human enzyme.
J Enzyme Inhib Med Chem 19: 17-32 (2004)
Saarland University
Pharmacological characterization of human S1P4 using a novel radioligand, [4,5-3H]-dihydrosphingosine-1-phosphate.
Br J Pharmacol 142: 851-60 (2004)
Schering-Plough Research Institute
Novel pyridazino[4,3-b]indoles with dual inhibitory activity against Mycobacterium tuberculosis and monoamine oxidase.
J Med Chem 47: 3455-61 (2004)
Russian Academy of Sciences
Selective inhibition of Trypanosoma brucei 6-phosphogluconate dehydrogenase by high-energy intermediate and transition-state analogues.
J Med Chem 47: 3427-37 (2004)
Cardiff University
Hybrids of [TSAO-T]-[foscarnet]: The first conjugate of foscarnet with a non-nucleoside reverse transcriptase inhibitor through a labile covalent ester bond.
J Med Chem 47: 3418-26 (2004)
Instituto De QuíMica MéDica (Csic)
On the function of the 14 A long internal cavity of histone deacetylase-like protein: implications for the design of histone deacetylase inhibitors.
J Med Chem 47: 3409-17 (2004)
University of Notre Dame
Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
J Med Chem 47: 3388-98 (2004)
National Institute On Drug Abuse-Intramural Research Program
Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.
J Med Chem 47: 3381-7 (2004)
Glaxosmithkline
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.
J Med Chem 47: 3367-80 (2004)
Pharmacia Italia
Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs.
J Med Chem 47: 3353-66 (2004)
Linkoping University
Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine.
Eur J Pharmacol 492: 123-30 (2004)
Memorial Sloan-Kettering Cancer Center
A mild, efficient and alpha-selective glycosidation by using potassium dodecatungstocobaltate trihydrate as catalyst.
Bioorg Med Chem Lett 14: 3611-4 (2004)
University of Isfahan
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.
Bioorg Med Chem Lett 14: 3601-5 (2004)
Novartis Institutes For Biomedical Research
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Bioorg Med Chem Lett 14: 3595-9 (2004)
Novartis Institutes For Biomedical Research
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Bioorg Med Chem Lett 14: 3589-93 (2004)
Merck Research Laboratories
Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines.
Bioorg Med Chem Lett 14: 3585-8 (2004)
Eli Lilly
An aminomethylpyrimidine DPP-IV inhibitor with improved properties.
Bioorg Med Chem Lett 14: 3575-8 (2004)
F. Hoffmann-La Roche
Phosphonate inhibitors of antigen 85C, a crucial enzyme involved in the biosynthesis of the Mycobacterium tuberculosis cell wall.
Bioorg Med Chem Lett 14: 3559-62 (2004)
University of Ljubljana
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.
Bioorg Med Chem Lett 14: 3549-53 (2004)
Bristol-Myers Squibb
Pseudodeflectusin, a novel isochroman derivative from Aspergillus pseudodeflectus a parasite of the sea weed, Sargassum fusiform, as a selective human cancer cytotoxin.
Bioorg Med Chem Lett 14: 3539-43 (2004)
Tokyo University of Science
Synthesis and evaluation of aminophosphinic acid derivatives as inhibitors of renal dipeptidase.
Bioorg Med Chem Lett 14: 3531-3 (2004)
The Sidney Kimmel Comprehensive Cancer Center At Johns Hopkins
BMS-201620: a selective beta 3 agonist.
Bioorg Med Chem Lett 14: 3525-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators.
Bioorg Med Chem Lett 14: 3521-3 (2004)
Institut Henri Beaufour
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
Bioorg Med Chem Lett 14: 3507-11 (2004)
Research Institute of Tsinghua University
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Bioorg Med Chem Lett 14: 3501-5 (2004)
Merck Research Laboratories
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Bioorg Med Chem Lett 14: 3495-9 (2004)
Merck Research Laboratories
Synthesis and anti-inflammatory effects of novel pimarane diterpenoid analogs.
Bioorg Med Chem Lett 14: 3487-90 (2004)
Seoul National University
Synthesis and biological activity of some known and putative duloxetine metabolites.
Bioorg Med Chem Lett 14: 3481-6 (2004)
Eli Lilly
Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1.
Bioorg Med Chem Lett 14: 3477-80 (2004)
Wyeth Research
Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid.
Bioorg Med Chem Lett 14: 3473-6 (2004)
Oxford University
Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.
Bioorg Med Chem Lett 14: 3457-60 (2004)
Wyeth Research
Synthesis of S-alkyl L-homocysteine analogues of glutathione and their kinetic studies with gamma-glutamyl transpeptidase.
Bioorg Med Chem Lett 14: 3451-5 (2004)
University of Montreal
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
Bioorg Med Chem Lett 14: 3441-4 (2004)
Merck Sharp & Dohme Research Laboratories
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Bioorg Med Chem Lett 14: 3425-9 (2004)
Glaxosmithkline
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Bioorg Med Chem Lett 14: 3419-24 (2004)
Merck Research Laboratories
Binding modes of 6,7 di-substituted 4-anilinoquinoline-3-carbonitriles to EGFR.
Bioorg Med Chem Lett 14: 3397-400 (2004)
Georgetown University
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
Bioorg Med Chem Lett 14: 3389-95 (2004)
Pfizer
6-Arylamino-7-chloro-quinazoline-5,8-diones as novel cytotoxic and DNA topoisomerase inhibitory agents.
Bioorg Med Chem Lett 14: 3385-8 (2004)
Ewha Womans University
3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.
Bioorg Med Chem Lett 14: 3379-84 (2004)
Institute of Science & Technology
Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.
NA
Wyeth Research
Ligand-directed functional heterogeneity of histamine H1 receptors: novel dual-function ligands selectively activate and block H1-mediated phospholipase C and adenylyl cyclase signaling.
J Pharmacol Exp Ther 311: 274-81 (2004)
University of North Carolina at Chapel Hill
Thioether metabolites of 3,4-methylenedioxyamphetamine and 3,4-methylenedioxymethamphetamine inhibit human serotonin transporter (hSERT) function and simultaneously stimulate dopamine uptake into hSERT-expressing SK-N-MC cells.
J Pharmacol Exp Ther 311: 298-306 (2004)
University of Texas At Austin
Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier.
Endocrinology 145: 4384-91 (2004)
The University of Tokyo
A new ursane triterpene from Monochaetum vulcanicum that inhibits DNA polymerase beta lyase.
J Nat Prod 67: 899-901 (2004)
Virginia Polytechnic Institute and State University
Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.
J Nat Prod 67: 872-4 (2004)
Merck Research Laboratories
Glycosidase-inhibiting pyrrolidines and pyrrolizidines with a long side chain in Scilla peruviana.
J Nat Prod 67: 846-50 (2004)
Hokuriku University
A new antimalarial quassinoid from Simaba orinocensis.
J Nat Prod 67: 772-7 (2004)
University of Mississippi
Molecular-targeted antitumor agents: the Saururus cernuus dineolignans manassantin B and 4-O-demethylmanassantin B are potent inhibitors of hypoxia-activated HIF-1.
J Nat Prod 67: 767-71 (2004)
University of Mississippi
2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution.
J Med Chem 47: 3320-3 (2004)
Astrazeneca R&D Charnwood
Design, synthesis, and structure-activity relationships of haloenol lactones: site-directed and isozyme-selective glutathione S-transferase inhibitors.
J Med Chem 47: 3282-94 (2004)
Chinese Academy of Sciences
Targeting the polyamine pathway with transition-state analogue inhibitors of 5'-methylthioadenosine phosphorylase.
J Med Chem 47: 3275-81 (2004)
Industrial Research
Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.
J Med Chem 47: 3264-74 (2004)
University College London
(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
J Med Chem 47: 3255-63 (2004)
Merck Research Laboratories
Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands.
J Med Chem 47: 3248-54 (2004)
National Cancer Institute At Frederick
Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.
J Med Chem 47: 3242-7 (2004)
University of Innsbruck
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.
J Med Chem 47: 3236-41 (2004)
Vanderbilt University School of Medicine
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
J Med Chem 47: 3220-35 (2004)
Abbott Laboratories
Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi.
J Med Chem 47: 3212-9 (2004)
University of California San Francisco
Conformationally constrained peptide analogues of pTyr-Glu-Glu-Ile as inhibitors of the Src SH2 domain binding.
J Med Chem 47: 3131-41 (2004)
University of Rhode Island
Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein interactions.
J Med Chem 47: 3111-30 (2004)
Sunesis Pharmaceuticals
New series of morpholine and 1,4-oxazepane derivatives as dopamine D4 receptor ligands: synthesis and 3D-QSAR model.
J Med Chem 47: 3089-104 (2004)
Neurosearch
Characterization of a ligand-receptor binding event using receptor-dependent four-dimensional quantitative structure-activity relationship analysis.
J Med Chem 47: 3075-88 (2004)
The University of Illinois At Chicago
A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations.
J Med Chem 47: 3065-74 (2004)
University of California San Francisco
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
J Med Chem 47: 3019-31 (2004)
Università
Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring.
J Med Chem 47: 3009-18 (2004)
University of Illinois At Chicago
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
J Med Chem 47: 2995-3008 (2004)
Merck Research Laboratories
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
J Med Chem 47: 2984-94 (2004)
University of Queensland
Sultam hydroxamates as novel matrix metalloproteinase inhibitors.
J Med Chem 47: 2981-3 (2004)
Bristol-Myers Squibb
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
J Med Chem 47: 2973-6 (2004)
Sri International
A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers.
J Med Chem 47: 2969-72 (2004)
University of Minnesota
High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter.
Mol Pharmacol 65: 1485-95 (2004)
Membrane Research Group of The Hungarian Academy of Sciences
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
Bioorg Med Chem Lett 14: 3351-5 (2004)
Merck Research Laboratories
N2-benzyl-N1-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamines and conformationally restrained indole analogues: development of calindol as a new calcimimetic acting at the calcium sensing receptor.
Bioorg Med Chem Lett 14: 3345-9 (2004)
Upr 2301 Centre National De La Recherche Scientifique
Thiol-based SAHA analogues as potent histone deacetylase inhibitors.
Bioorg Med Chem Lett 14: 3313-7 (2004)
Nagoya City University
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
Bioorg Med Chem Lett 14: 3307-12 (2004)
F. Hoffmann-La Roche
New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.
Bioorg Med Chem Lett 14: 3303-6 (2004)
Pfizer
The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor.
Bioorg Med Chem Lett 14: 3295-8 (2004)
National Institute On Drug Abuse-Intramural Research Program
Design and synthesis of dysidiolide analogs from vitamin D3: novel class of Cdc25A inhibitors.
Bioorg Med Chem Lett 14: 3291-4 (2004)
The University of Tokyo
Carbonic anhydrase inhibitors: the first QSAR study on inhibition of tumor-associated isoenzyme IX with aromatic and heterocyclic sulfonamides.
Bioorg Med Chem Lett 14: 3283-90 (2004)
Laxmi Fumigation and Pest Control (P)
Long chain amines and long chain ammonium salts as novel inhibitors of dynamin GTPase activity.
Bioorg Med Chem Lett 14: 3275-8 (2004)
The University of Newcastle
2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: a novel class of small molecule heparanase inhibitors.
Bioorg Med Chem Lett 14: 3269-73 (2004)
Celltech R&D
A novel 18 beta-glycyrrhetinic acid analogue as a potent and selective inhibitor of 11 beta-hydroxysteroid dehydrogenase 2.
Bioorg Med Chem Lett 14: 3263-7 (2004)
University of Bath
The monoethyl ester of meconic acid is an active site inhibitor of HCV NS5B RNA-dependent RNA polymerase.
Bioorg Med Chem Lett 14: 3257-61 (2004)
Mrl Rome
Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.
Bioorg Med Chem Lett 14: 3251-6 (2004)
University of Ljubljana
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.
Bioorg Med Chem Lett 14: 3245-50 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.
Bioorg Med Chem Lett 14: 3235-40 (2004)
Pfizer
Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives.
Bioorg Med Chem Lett 14: 3231-4 (2004)
University of Kuopio
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
Bioorg Med Chem Lett 14: 3227-30 (2004)
Pfizer
Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
Bioorg Med Chem Lett 14: 3221-6 (2004)
University of Maryland
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 3217-20 (2004)
Eli Lilly
Development of l-3-aminotyrosine suitably protected for the synthesis of a novel nonphosphorylated hexapeptide with low-nanomolar Grb2-SH2 domain-binding affinity.
Bioorg Med Chem Lett 14: 3205-8 (2004)
Institute of Materia Medica
Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis.
Bioorg Med Chem Lett 14: 3195-9 (2004)
Merck Frosst Centre For Therapeutic Research
High-throughput identification of fucosyltransferase inhibitors using carbohydrate microarrays.
Bioorg Med Chem Lett 14: 3185-8 (2004)
The Scripps Research Institute
Design and synthesis of beta-amino-alpha-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth.
Bioorg Med Chem Lett 14: 3181-4 (2004)
Celera
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
Bioorg Med Chem Lett 14: 3173-6 (2004)
Fudan University
In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase.
Bioorg Med Chem Lett 14: 3155-9 (2004)
Bayer Research Center
Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.
Bioorg Med Chem Lett 14: 3143-6 (2004)
Johnson and Johnson Pharmaceutical Research and Development
2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents.
Bioorg Med Chem Lett 14: 3135-8 (2004)
University of Bath
Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy.
Bioorg Med Chem Lett 14: 3121-5 (2004)
Morphochem
Synthesis and activity of phosphinic tripeptide inhibitors of cathepsin C.
Bioorg Med Chem Lett 14: 3113-6 (2004)
Wroclaw University of Technology
Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis.
Bioorg Med Chem Lett 14: 3109-12 (2004)
Korea Research Institute of Bioscience and Biotechnology
SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)-N-(3-pyridinylmethyl)ethanesulfonamide.
Bioorg Med Chem Lett 14: 3099-102 (2004)
Eli Lilly
Molecular modeling studies on the active binding site of the blood-brain barrier choline transporter.
Bioorg Med Chem Lett 14: 3085-92 (2004)
Texas Tech University Health Sciences Center
A TOPS-MODE approach to predict adenosine kinase inhibition.
Bioorg Med Chem Lett 14: 3077-9 (2004)
Vigo University
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.
Bioorg Med Chem Lett 14: 3073-5 (2004)
Pfizer
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Bioorg Med Chem Lett 14: 3063-8 (2004)
Abbott Laboratories
Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 3057-61 (2004)
Eli Lilly
N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.
Bioorg Med Chem Lett 14: 3053-6 (2004)
Johnson & Johnson Pharmaceutical Research and Development
A novel series of potent and selective small molecule inhibitors of the complement component C1s.
Bioorg Med Chem Lett 14: 3043-7 (2004)
3-Dimensional Pharmaceuticals
Identification and optimization of novel partial agonists of neuromedin B receptor using parallel synthesis.
Bioorg Med Chem Lett 14: 3037-42 (2004)
Tularik
Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity.
Biochemistry 43: 6091-100 (2004)
Merck Research Laboratories
Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System.
J Pharmacol Exp Ther 311: 204-12 (2004)
Actelion Pharmaceuticals
3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects.
J Pharmacol Exp Ther 310: 620-32 (2004)
Bayer Healthcare
Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif.
J Med Chem 47: 2939-42 (2004)
IQM-CSIC
Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors.
J Med Chem 47: 2906-16 (2004)
University of Antwerp
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
J Med Chem 47: 2897-905 (2004)
National Health Research Institutes
Discovery of the first non-peptide full agonists for the human bradykinin B(2) receptor incorporating 4-(2-picolyloxy)quinoline and 1-(2-picolyl)benzimidazole frameworks.
J Med Chem 47: 2853-63 (2004)
Fujisawa Pharmaceutical
Interaction of cycloSal-pronucleotides with cholinesterases from different origins. A structure-activity relationship.
J Med Chem 47: 2839-52 (2004)
University of Hamburg
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
J Med Chem 47: 2833-8 (2004)
Novo Nordisk
Carbamoylphosphonates, a new class of in vivo active matrix metalloproteinase inhibitors. 1. Alkyl- and cycloalkylcarbamoylphosphonic acids.
J Med Chem 47: 2826-32 (2004)
The Hebrew University of Jerusalem
Incorporating molecular shape into the alignment-free Grid-Independent Descriptors.
J Med Chem 47: 2805-15 (2004)
Universitat Pompeu Fabra
Carbonic anhydrase inhibitors: synthesis and topical intraocular pressure lowering effects of fluorine-containing inhibitors devoid of enhanced reactivity.
J Med Chem 47: 2796-804 (2004)
Universita Degli Studi Di Firenze
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
J Med Chem 47: 2776-95 (2004)
Actelion Pharmaceuticals
BREED: Generating novel inhibitors through hybridization of known ligands. Application to CDK2, p38, and HIV protease.
J Med Chem 47: 2768-75 (2004)
Vertex Pharmaceuticals
Receptor flexibility in the in silico screening of reagents in the S1' pocket of human collagenase.
J Med Chem 47: 2761-7 (2004)
De Novo Pharmaceuticals
Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.
J Med Chem 47: 2750-60 (2004)
University of Innsbruck
Comparative molecular active site analysis (CoMASA). 1. An approach to rapid evaluation of 3D QSAR.
J Med Chem 47: 2732-42 (2004)
Nippon Zoki Pharmaceutical
Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors.
J Med Chem 47: 2728-31 (2004)
Fujisawa Pharmaceutical
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production.
J Med Chem 47: 2724-7 (2004)
Procter and Gamble Pharmaceuticals
Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse?
J Med Chem 47: 2717-23 (2004)
Hospital of The University of Pennsylvania
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
J Pharmacol Exp Ther 310: 905-14 (2004)
Sanofi-Synthelabo Recherche
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.
Bioorg Med Chem Lett 14: 2987-9 (2004)
Johnson and Johnson Pharmaceutical Research and Development
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.
Bioorg Med Chem Lett 14: 2973-7 (2004)
Bristol-Myers Squibb
Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C.
Bioorg Med Chem Lett 14: 2963-7 (2004)
Tohoku University
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Bioorg Med Chem Lett 14: 2955-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and characterization of an ATP-peptide conjugate inhibitor of protein kinase A.
Bioorg Med Chem Lett 14: 2951-4 (2004)
Johns Hopkins University School of Medicine
Synergetic inhibition of genistein and D-glucose on alpha-glucosidase.
Bioorg Med Chem Lett 14: 2947-50 (2004)
Sun Yat-Sen (Zhongshan) University
The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.
Bioorg Med Chem Lett 14: 2941-5 (2004)
Merck Research Laboratories
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.
Bioorg Med Chem Lett 14: 2935-9 (2004)
Daiichi Pharmaceutical
Plasmepsin II inhibition and antiplasmodial activity of Primaquine-Statine 'double-drugs'.
Bioorg Med Chem Lett 14: 2931-4 (2004)
University of Milan
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety.
Bioorg Med Chem Lett 14: 2917-22 (2004)
Janssen-Cilag
N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists.
Bioorg Med Chem Lett 14: 2905-9 (2004)
Amgen
Reverse hydroxamate-based selective TACE inhibitors.
Bioorg Med Chem Lett 14: 2897-900 (2004)
Kaken Pharmaceutical
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Bioorg Med Chem Lett 14: 2871-5 (2004)
Merck
Design, synthesis and structure-activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity.
Bioorg Med Chem Lett 14: 2857-62 (2004)
Dainippon Pharmaceutical
Silanediol peptidomimetics. Evaluation of four diastereomeric ACE inhibitors.
Bioorg Med Chem Lett 14: 2853-6 (2004)
State University of New York
PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues.
Bioorg Med Chem Lett 14: 2847-51 (2004)
Monash University
Solid-phase synthesis of kojic acid-tripeptides and their tyrosinase inhibitory activity, storage stability, and toxicity.
Bioorg Med Chem Lett 14: 2843-6 (2004)
Seoul National University
Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel.
Bioorg Med Chem Lett 14: 2823-7 (2004)
Aventis Pharma Deutschland
Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.
Bioorg Med Chem Lett 14: 2801-5 (2004)
Aventis Pharma Deutschland
2,4-Bis(octadecanoylamino)benzenesulfonic acid sodium salt as a novel scavenger receptor inhibitor with low molecular weight.
Bioorg Med Chem Lett 14: 2791-5 (2004)
Organon K.K.
Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.
Bioorg Med Chem Lett 14: 2765-71 (2004)
Janssen-Cilag
Design and synthesis of benzofused heterocyclic RXR modulators.
Bioorg Med Chem Lett 14: 2759-63 (2004)
Eli Lilly
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.
Bioorg Med Chem Lett 14: 2747-52 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Bioorg Med Chem Lett 14: 2741-5 (2004)
Merck Research Laboratories
Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist.
Bioorg Med Chem Lett 14: 2735-40 (2004)
University of Virginia
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.
Bioorg Med Chem Lett 14: 2729-33 (2004)
Pfizer
Synthesis and target identification of hymenialdisine analogs.
Chem Biol 11: 247-59 (2004)
Genomics Institute of The Novartis Research Foundation
Systems-based design of bi-ligand inhibitors of oxidoreductases: filling the chemical proteomic toolbox.
Chem Biol 11: 185-94 (2004)
Triad Therapeutics
Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.
Chem Biol 11: 525-34 (2004)
Cyclacel
Lobeline analogs with enhanced affinity and selectivity for plasmalemma and vesicular monoamine transporters.
J Pharmacol Exp Ther 310: 1035-45 (2004)
University of Kentucky
Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity.
J Biol Chem 279: 31429-39 (2004)
University of Bristol
[1-(3,5-difluoro-4-hydroxyphenyl)-1H-pyrrol-3-yl]phenylmethanone as a bioisostere of a carboxylic acid aldose reductase inhibitor.
J Med Chem 47: 2706-9 (2004)
Aristotle University of Thessaloniki
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
J Med Chem 47: 2678-87 (2004)
Freie UniversitäT Berlin
A new class of nonpeptide bradykinin B(2) receptor ligand, incorporating a 4-aminoquinoline framework. Identification of a key pharmacophore to determine species difference and agonist/antagonist profile.
J Med Chem 47: 2667-77 (2004)
Fujisawa Pharmaceutical
New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.
J Med Chem 47: 2659-66 (2004)
Collegium Medicum of The Jagiellonian University
Inhibitors of Sir2: evaluation of splitomicin analogues.
J Med Chem 47: 2635-44 (2004)
Fred Hutchinson Cancer Research Center
Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
J Med Chem 47: 2624-34 (2004)
National Institute of Diabetes and Digestive and Kidney Diseases
Oral bioavailability of a new class of micro-opioid receptor agonists containing 3,6-bis[Dmt-NH(CH(2))(n)]-2(1H)-pyrazinone with central-mediated analgesia.
J Med Chem 47: 2599-610 (2004)
National Institutes of Environmental Health Sciences
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
J Med Chem 47: 2587-98 (2004)
Pharmaceutical Research Institute
Design, synthesis, structural studies, biological evaluation, and computational simulations of novel potent AT(1) angiotensin II receptor antagonists based on the 4-phenylquinoline structure.
J Med Chem 47: 2574-86 (2004)
Università
Rational design and synthesis of novel dimeric diketoacid-containing inhibitors of HIV-1 integrase: implication for binding to two metal ions on the active site of integrase.
J Med Chem 47: 2561-73 (2004)
Institute of Materia Medica
General model for estimation of the inhibition of protein kinases using Monte Carlo simulations.
J Med Chem 47: 2534-49 (2004)
Yale University
Non-peptidic small-molecule inhibitors of the single-chain hepatitis C virus NS3 protease/NS4A cofactor complex discovered by structure-based NMR screening.
J Med Chem 47: 2486-98 (2004)
Schering-Plough Research Institute
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.
J Med Chem 47: 2475-85 (2004)
Harvard Medical School
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.
J Med Chem 47: 2466-74 (2004)
Merck Research Laboratories
5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential probes for imaging with positron emission tomog
J Med Chem 47: 2453-65 (2004)
National Institute On Drug Abuse
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.
J Med Chem 47: 2441-52 (2004)
Merck Research Laboratories
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
J Med Chem 47: 2430-40 (2004)
University of Michigan Comprehensive Cancer Center
N-phenylphenylglycines as novel corticotropin releasing factor receptor antagonists.
J Med Chem 47: 2426-9 (2004)
Bristol-Myers Squibb Pharma Research Laboratories
Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists.
J Med Chem 47: 2422-5 (2004)
Eli Lilly
Discovery of diarylacrylonitriles as a novel series of small molecule sortase A inhibitors.
J Med Chem 47: 2418-21 (2004)
Seoul National University
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.
J Med Chem 47: 2411-3 (2004)
University of Antwerp
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagoni
J Med Chem 47: 2405-8 (2004)
Schering-Plough Research Institute
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.
Bioorg Med Chem Lett 14: 2685-91 (2004)
Idun Pharmaceuticals
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4.
Bioorg Med Chem Lett 14: 2653-6 (2004)
Eli Lilly
Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia.
Bioorg Med Chem Lett 14: 2617-20 (2004)
The University of Tokyo
A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.
Bioorg Med Chem Lett 14: 2613-6 (2004)
Abbott Bioresearch Center
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.
Bioorg Med Chem Lett 14: 2603-7 (2004)
Wyeth Research
S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates as CETP inhibitors.
Bioorg Med Chem Lett 14: 2589-91 (2004)
Central Pharmaceutical Research Institute
Synthesis of 1alpha,25-dihydroxyvitamin D3-26,23-lactams (DLAMs), a novel series of 1 alpha,25-dihydroxyvitamin D3 antagonist.
Bioorg Med Chem Lett 14: 2579-83 (2004)
University of Tokyo
Discovery of a potent and selective alpha v beta 3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model.
Bioorg Med Chem Lett 14: 2567-70 (2004)
Dainippon Pharmaceutical
Simple aromatic compounds containing propenone moiety show considerable dual COX/5-LOX inhibitory activities.
Bioorg Med Chem Lett 14: 2559-62 (2004)
Yeungnam University
Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.
Bioorg Med Chem Lett 14: 2551-4 (2004)
Merck Research Laboratories
Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 14: 2543-6 (2004)
Glaxosmithkline
Rational design and synthesis of novel heparan sulfate mimetic compounds as antiadhesive agents.
Bioorg Med Chem Lett 14: 2505-9 (2004)
Riken Discovery Research Institute
Design and synthesis of bridged gamma-lactams as analogues of beta-lactam antibiotics.
Bioorg Med Chem Lett 14: 2489-92 (2004)
Aventis Pharma
Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain.
Bioorg Med Chem Lett 14: 2483-7 (2004)
Novartis Institutes For Biomedical Research
Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides.
Bioorg Med Chem Lett 14: 2477-81 (2004)
University College London
Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity.
Bioorg Med Chem Lett 14: 2473-6 (2004)
Cnrs Umr 8076
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Bioorg Med Chem Lett 14: 2469-72 (2004)
Eli Lilly
Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel.
Bioorg Med Chem Lett 14: 2463-7 (2004)
Merck Research Laboratories
Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists.
Bioorg Med Chem Lett 14: 2451-7 (2004)
Novartis Pharma
Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands.
Bioorg Med Chem Lett 14: 2443-6 (2004)
Otsuka Pharmaceutical Factory
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.
Bioorg Med Chem Lett 14: 2433-7 (2004)
University of Newcastle
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
Bioorg Med Chem Lett 14: 2427-31 (2004)
Institute of Technology
Different regulation of human delta-opioid receptors by SNC-80 [(+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide] and endogenous enkephalins.
J Pharmacol Exp Ther 310: 666-77 (2004)
Laboratoire De Biochimie A
Development of bombesin analogs with conformationally restricted amino acid substitutions with enhanced selectivity for the orphan receptor human bombesin receptor subtype 3.
J Pharmacol Exp Ther 310: 1161-70 (2004)
National Institutes of Health
Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
J Pharmacol Exp Ther 310: 943-51 (2004)
Acadia Pharmaceuticals
Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.
J Med Chem 47: 2375-88 (2004)
Medical College of Ohio
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
J Med Chem 47: 2348-55 (2004)
Abbott Laboratories
Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX.
J Med Chem 47: 2337-47 (2004)
Canadian Institutes of Health Research
Khellinone derivatives as blockers of the voltage-gated potassium channel Kv1.3: synthesis and immunosuppressive activity.
J Med Chem 47: 2326-36 (2004)
Institute of Medical Research Biotechnology Centre
4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.
J Med Chem 47: 2308-17 (2004)
Università
Structure-activity relationship of purine ribonucleosides for inhibition of hepatitis C virus RNA-dependent RNA polymerase.
J Med Chem 47: 2283-95 (2004)
Isis Pharmaceuticals
Heterocyclic bis-cations as starting hits for design of inhibitors of the bifunctional enzyme histidine-containing protein kinase/phosphatase from Bacillus subtilis.
J Med Chem 47: 2264-75 (2004)
University of Strasburg
Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative.
J Med Chem 47: 2243-55 (2004)
University of Bonn
Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain.
J Med Chem 47: 2228-35 (2004)
National Institute of Radiological Sciences
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
J Med Chem 47: 2194-207 (2004)
University of Florida
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
J Med Chem 47: 2180-93 (2004)
Nitromed
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
J Med Chem 47: 2176-9 (2004)
Merck Sharp and Dohme Research Laboratories
Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.
J Med Chem 47: 2171-5 (2004)
Merck Research Laboratories
Inhibition of fucosyltransferase VII by gallic acid and its derivatives.
Arch Biochem Biophys 425: 51-7 (2004)
Schering-Plough Research Institute
Indoline derivatives as 5-HT(2C) receptor agonists.
Bioorg Med Chem Lett 14: 2367-70 (2004)
Vernalis Research
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a topically acting antiglaucoma sulfonamide.
Bioorg Med Chem Lett 14: 2357-61 (2004)
Bruker-Axs
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered.
Bioorg Med Chem Lett 14: 2351-6 (2004)
Universita Degli Studi Di Firenze
3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Bioorg Med Chem Lett 14: 2345-9 (2004)
Universita Degli Studi Di Firenze
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4.
Bioorg Med Chem Lett 14: 2331-4 (2004)
Merck Research Laboratories
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.
Bioorg Med Chem Lett 14: 2327-30 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Amidines as amide bond replacements in VLA-4 antagonists.
Bioorg Med Chem Lett 14: 2323-6 (2004)
Merck Research Laboratories
Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta.
Bioorg Med Chem Lett 14: 2303-8 (2004)
Cell Therapeutics
Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic activity.
Bioorg Med Chem Lett 14: 2291-7 (2004)
Seoul National University
Tight binding ligand approach to oligosaccharide-grafted protein.
Bioorg Med Chem Lett 14: 2285-9 (2004)
Jst
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).
Bioorg Med Chem Lett 14: 2279-83 (2004)
Virginia Commonwealth University
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.
Bioorg Med Chem Lett 14: 2269-74 (2004)
Neurocrine Biosciences
5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.
Bioorg Med Chem Lett 14: 2265-8 (2004)
Ucb Pharma
Novel halogenated nitrobenzylthioinosine analogs as es nucleoside transporter inhibitors.
Bioorg Med Chem Lett 14: 2257-60 (2004)
University of Tennessee Health Sciences Center
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 2249-52 (2004)
Astrazeneca
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 2245-8 (2004)
Astrazeneca
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
Bioorg Med Chem Lett 14: 2233-9 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.
Bioorg Med Chem Lett 14: 2227-31 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Application of the four-component Ugi condensation for the preparation of sulfated glycoconjugate libraries.
Bioorg Med Chem Lett 14: 2221-6 (2004)
Progen Industries
Thioxanthene-derived analogs as sigma(1) receptor ligands.
Bioorg Med Chem Lett 14: 2217-20 (2004)
Virginia Commonwealth University
Discovery of novel nonsteroidal glucocorticoid receptor modulators.
Bioorg Med Chem Lett 14: 2209-12 (2004)
Abbott Laboratories
Structure-activity relationships of novel inhibitors of glyceraldehyde-3-phosphate dehydrogenase.
Bioorg Med Chem Lett 14: 2199-204 (2004)
Universidade Federal De Minas Gerais
2,3-diarylpyran-4-ones: a new series of selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 2195-8 (2004)
Pharmaceutical & Health Research Institute
Novel pyrrole-containing progesterone receptor modulators.
Bioorg Med Chem Lett 14: 2185-9 (2004)
Wyeth Research
Novel CCR1 antagonists with improved metabolic stability.
Bioorg Med Chem Lett 14: 2175-9 (2004)
Pfizer
Potent small molecule CCR1 antagonists.
Bioorg Med Chem Lett 14: 2169-73 (2004)
Pfizer
The discovery of structurally novel CCR1 antagonists derived from a hydroxyethylene peptide isostere template.
Bioorg Med Chem Lett 14: 2163-7 (2004)
Pfizer
Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles.
Bioorg Med Chem Lett 14: 2155-8 (2004)
Wyeth Research
Capped dipeptide phenethylamide inhibitors of the HCV NS3 protease.
Bioorg Med Chem Lett 14: 2151-4 (2004)
Irbm, Mrl Rome
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.
Bioorg Med Chem Lett 14: 2141-5 (2004)
Merck Research Laboratories
Didehydrofarnesyl diphosphate: an intrinsically fluorescent inhibitor of protein farnesyltransferase.
Bioorg Med Chem Lett 14: 2137-40 (2004)
The University of Utah
Novel GSK-3 inhibitors with improved cellular activity.
Bioorg Med Chem Lett 14: 2127-30 (2004)
Glaxosmithkline
Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors.
Bioorg Med Chem Lett 14: 2121-5 (2004)
Glaxosmithkline
Synthesis and monoamine transporter affinity of 3'-analogs of 2-beta-carbomethoxy-3-beta-(4'-iodophenyl)tropane (beta-CIT).
Bioorg Med Chem Lett 14: 2117-20 (2004)
Yale School of Medicine
N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address.
Bioorg Med Chem Lett 14: 2113-6 (2004)
Johnson and Johnson Pharmaceutical Research and Development
N,N-dialkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, potent, selective delta opioid agonists.
Bioorg Med Chem Lett 14: 2109-12 (2004)
Johnson and Johnson Pharmaceutical Research and Development
Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring.
Bioorg Med Chem Lett 14: 2099-103 (2004)
Ewha Womans University
Synthesis of fluorinated cyclopentenyladenine as potent inhibitor of S-adenosylhomocysteine hydrolase.
Bioorg Med Chem Lett 14: 2091-3 (2004)
Ewha Womans University
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.
Bioorg Med Chem Lett 14: 2083-6 (2004)
Neurocrine Biosciences
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Bioorg Med Chem Lett 14: 2079-82 (2004)
Abbott Laboratories
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.
Bioorg Med Chem Lett 14: 2073-8 (2004)
Millennium Pharmaceuticals
N-Benzoyl amino acids as ICAM/LFA-1 inhibitors. Part 2: structure-activity relationship of the benzoyl moiety.
Bioorg Med Chem Lett 14: 2055-9 (2004)
Genentech
Biaryl amide glucagon receptor antagonists.
Bioorg Med Chem Lett 14: 2047-50 (2004)
Abbott Laboratories
The design, preparation and SAR of novel small molecule sodium (Na(+)) channel blockers.
Bioorg Med Chem Lett 14: 2025-30 (2004)
Arqule
Characterization of two novel N-methyl-D-aspartate antagonists: EAA-090 (2-[8,9-dioxo-2,6-diazabicyclo [5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride).
J Pharmacol Exp Ther 310: 563-70 (2004)
Wyeth Research
Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro.
Cancer Res 64: 2333-7 (2004)
St. Jude Children'S Research Hospital
Macrocyclization in the design of non-phosphorus-containing Grb2 SH2 domain-binding ligands.
J Med Chem 47: 2166-9 (2004)
National Cancer Institute-Frederick
Design, synthesis, and biological activity of 1,3-disubstituted ureas as potent inhibitors of the soluble epoxide hydrolase of increased water solubility.
J Med Chem 47: 2110-22 (2004)
University of California Davis
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
J Med Chem 47: 2089-96 (2004)
Merck Research Laboratories
Synthesis and selective inhibitory activity of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives against monoamine oxidase.
J Med Chem 47: 2071-4 (2004)
Sapienza University of Rome
Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists.
J Med Chem 47: 2037-61 (2004)
Millennium Pharmaceuticals
A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution.
J Med Chem 47: 2030-6 (2004)
Academy of Sciences of The Czech Republic
Structure-based design of potent retinoid X receptor alpha agonists.
J Med Chem 47: 2010-29 (2004)
Glaxosmithkline
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
J Med Chem 47: 1969-86 (2004)
Encysive Pharmaceuticals
Identification of compounds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening.
J Med Chem 47: 1962-8 (2004)
Astrazeneca
Crystal structures of the vitamin D nuclear receptor liganded with the vitamin D side chain analogues calcipotriol and seocalcitol, receptor agonists of clinical importance. Insights into a structural basis for the switching of calcipotriol to a receptor antagonist by further side chain modificatio
J Med Chem 47: 1956-61 (2004)
Institute of Genetics and Molecular and Cellular Biology (Igbmc)
Orally bioavailable competitive CCR5 antagonists.
J Med Chem 47: 1939-55 (2004)
Novartis Institutes For Biomedical Research
Azasugar-based MMP/ADAM inhibitors as antipsoriatic agents.
J Med Chem 47: 1930-8 (2004)
Hokkaido Collaboration Center N-21
Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives.
J Med Chem 47: 1919-29 (2004)
Biocryst Pharmaceuticals
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.
J Med Chem 47: 1900-18 (2004)
Recordati
Design and syntheses of 1,6-naphthalene derivatives as selective HCMV protease inhibitors.
J Med Chem 47: 1893-9 (2004)
Wyeth Research
Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases.
J Med Chem 47: 1889-92 (2004)
School of Chemistry and Biochemistry and The Parker H. Petit Institute For Bioengineering and Bioscience
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
J Med Chem 47: 1886-8 (2004)
Harvard Medical School
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
J Med Chem 47: 1869-78 (2004)
Merck Research Laboratories
DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.
J Pharmacol Exp Ther 310: 783-92 (2004)
Purdue Pharma Discovery Research
In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase.
NA
Novartis Institutes for BioMedical Research
Discovery and optimization of 2-aryl oxazolo-pyrimidines as adenosine kinase inhibitors using liquid phase parallel synthesis.
Bioorg Med Chem Lett 14: 1997-2000 (2004)
Bayer
(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.
Bioorg Med Chem Lett 14: 1991-5 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Parallel synthesis of DAPT derivatives and their gamma-secretase-inhibitory activity.
Bioorg Med Chem Lett 14: 1983-5 (2004)
University of Tokyo
Structure-activity relationships of untenone A and its derivatives for inhibition of DNA polymerases.
Bioorg Med Chem Lett 14: 1975-7 (2004)
Tokyo University of Science
Modified norcantharidins; synthesis, protein phosphatases 1 and 2A inhibition, and anticancer activity.
Bioorg Med Chem Lett 14: 1969-73 (2004)
University of California Irvine
1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands.
Bioorg Med Chem Lett 14: 1961-4 (2004)
Virginia Commonwealth University
Sulfonamido, azidosulfonyl and N-acetylsulfonamido analogues of rofecoxib: 4-[4-(N-acetylsulfonamido)phenyl]-3-(4-methanesulfonylphenyl)-2(5H)furanone is a potent and selective cyclooxygenase-2 inhibitor.
Bioorg Med Chem Lett 14: 1957-60 (2004)
University of Alberta
Design of acyclic triaryl olefins: a new class of potent and selective cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 1953-6 (2004)
University of Alberta
Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants.
Bioorg Med Chem Lett 14: 1939-42 (2004)
Vertex Pharmaceuticals
Probing pockets S2-S4' of the gamma-secretase active site with (hydroxyethyl)urea peptidomimetics.
Bioorg Med Chem Lett 14: 1935-8 (2004)
Harvard Medical School
Farnesyloxycoumarins, a new class of squalene-hopene cyclase inhibitors.
Bioorg Med Chem Lett 14: 1931-4 (2004)
Università
Evans Blue and other dyes as protein tyrosine phosphatase inhibitors.
Bioorg Med Chem Lett 14: 1923-6 (2004)
Inha University
Hydroxytriamides as potent gamma-secretase inhibitors.
Bioorg Med Chem Lett 14: 1917-21 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.
Bioorg Med Chem Lett 14: 1913-6 (2004)
Merck Research Laboratories
Potent and selective inhibitors of bacterial methionyl tRNA synthetase derived from an oxazolone-dipeptide scaffold.
Bioorg Med Chem Lett 14: 1909-11 (2004)
Arqule
Epibatidine structure-activity relationships.
Bioorg Med Chem Lett 14: 1889-96 (2004)
Research Triangle Institute
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
Bioorg Med Chem Lett 14: 1879-87 (2004)
University of Maryland
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
Bioorg Med Chem Lett 14: 1869-74 (2004)
University of Kentucky
Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents.
Bioorg Med Chem Lett 14: 1863-7 (2004)
University of Kentucky
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 14: 1855-8 (2004)
University of Illinois At Chicago
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
Bioorg Med Chem Lett 14: 1849-53 (2004)
University of Florida
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Bioorg Med Chem Lett 14: 1845-8 (2004)
Georgetown University School of Medicine
alpha4beta2 nACh receptor pharmacophore models.
Bioorg Med Chem Lett 14: 1841-4 (2004)
Virginia Commonwealth University
Inhibitor binding in a class 2 dihydroorotate dehydrogenase causes variations in the membrane-associated N-terminal domain.
Protein Sci 13: 1031-42 (2004)
University of Copenhagen
Antityrosinase principles and constituents of the petals of Crocus sativus.
J Nat Prod 67: 437-40 (2004)
National Cheng Kung University
Effects of natural flavones and flavonols on the kinase activity of Cdk5.
J Nat Prod 67: 416-20 (2004)
University of Chile
Iridoids as allelochemicals and DNA polymerase inhibitors.
J Nat Prod 67: 357-61 (2004)
Universidad Nacional De San Luis
Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.
Eur J Pharmacol 487: 183-97 (2004)
Abbott Laboratories
Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2.
J Med Chem 47: 1864-7 (2004)
Vrije Universiteit Brussel
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
J Med Chem 47: 1852-5 (2004)
University of Pisa
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
J Med Chem 47: 1807-22 (2004)
Merck Sharp and Dohme Research Laboratories
Fluorinated phenylcyclopropylamines. 1. Synthesis and effect of fluorine substitution at the cyclopropane ring on inhibition of microbial tyramine oxidase.
J Med Chem 47: 1796-806 (2004)
National Institute of Diabetes and Digestive and Kidney Diseases
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
J Med Chem 47: 1760-6 (2004)
Emory University
Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents.
J Med Chem 47: 1729-38 (2004)
University of Illinois At Chicago
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.
J Med Chem 47: 1719-28 (2004)
Bristol-Myers Squibb
Discovery of a potent and novel motilin agonist.
J Med Chem 47: 1704-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Validation of molecular docking calculations involving FGF-1 and FGF-2.
J Med Chem 47: 1683-93 (2004)
Progen Industries
Synthesis and monoamine transporter binding of 2-(diarylmethoxymethyl)-3 beta-aryltropane derivatives.
J Med Chem 47: 1676-82 (2004)
University of New Orleans
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.
J Med Chem 47: 1662-75 (2004)
Cyclacel
Unraveling the active conformation of urotensin II.
J Med Chem 47: 1652-61 (2004)
University of Salerno
Countering cooperative effects in protease inhibitors using constrained beta-strand-mimicking templates in focused combinatorial libraries.
J Med Chem 47: 1641-51 (2004)
The University of Queensland
A new series of highly potent non-peptide bradykinin B2 receptor antagonists incorporating the 4-heteroarylquinoline framework. Improvement of aqueous solubility and new insights into species difference.
J Med Chem 47: 1617-30 (2004)
Fujisawa Pharmaceutical
Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.
J Med Chem 47: 1602-4 (2004)
Millennium Pharmaceuticals
7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases.
J Med Chem 47: 1599-601 (2004)
Wyeth Research
Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.
Bioorg Med Chem Lett 14: 1811-5 (2004)
Harvard Medical School
Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan.
Bioorg Med Chem Lett 14: 1807-9 (2004)
Ucb Pharma
Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites.
Bioorg Med Chem Lett 14: 1799-802 (2004)
State University of New York
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.
Bioorg Med Chem Lett 14: 1795-8 (2004)
Merck
Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists.
Bioorg Med Chem Lett 14: 1791-4 (2004)
Schering-Plough Research Institute
Synthesis and evaluation of substituted 4-alkoxy-2-aminopyridines as novel neuropeptide Y1 receptor antagonists.
Bioorg Med Chem Lett 14: 1761-4 (2004)
Tsukuba Research Institute
A prodrug approach to COX-2 inhibitors with methylsulfone.
Bioorg Med Chem Lett 14: 1757-60 (2004)
Amorepacific
6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays.
Bioorg Med Chem Lett 14: 1745-9 (2004)
Sapienza University of Rome
Carbazates as potent inhibitors of hormone-sensitive lipase.
Bioorg Med Chem Lett 14: 1741-4 (2004)
Novo Nordisk
The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.
Bioorg Med Chem Lett 14: 1737-9 (2004)
University of Huddersfield
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.
Bioorg Med Chem Lett 14: 1721-7 (2004)
Abbott Laboratories
Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesis.
Bioorg Med Chem Lett 14: 1717-20 (2004)
Pharmacopeia
Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis.
Bioorg Med Chem Lett 14: 1713-6 (2004)
Pharmacopeia
The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands.
Bioorg Med Chem Lett 14: 1709-12 (2004)
Arqule
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.
Bioorg Med Chem Lett 14: 1703-7 (2004)
Cnrs
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.
Bioorg Med Chem Lett 14: 1693-6 (2004)
Seoul National University
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 1683-8 (2004)
Discovery Research-Dr. Reddy'S Laboratories
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.
Bioorg Med Chem Lett 14: 1679-82 (2004)
The Neuroscience Research Centre
Design and synthesis of macrocyclic inhibitors of phosphatase cdc25B.
Bioorg Med Chem Lett 14: 1673-7 (2004)
Schering
Inhibitory activities against topoisomerase I and II by polyhydroxybenzoyl amide derivatives and their structure-activity relationship.
Bioorg Med Chem Lett 14: 1669-72 (2004)
Kumamoto University
Synthesis and evaluation of analogues of S-adenosyl-L-methionine, as inhibitors of the E. coli cyclopropane fatty acid synthase.
Bioorg Med Chem Lett 14: 1661-4 (2004)
Pierre and Marie Curie University
Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.
Bioorg Med Chem Lett 14: 1655-9 (2004)
Roche Palo Alto
Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.
Bioorg Med Chem Lett 14: 1645-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists.
Bioorg Med Chem Lett 14: 1619-24 (2004)
Array Biopharma
The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.
Bioorg Med Chem Lett 14: 1615-8 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
[3H]A-317491, a novel high-affinity non-nucleotide antagonist that specifically labels human P2X2/3 and P2X3 receptors.
J Pharmacol Exp Ther 310: 407-16 (2004)
Abbott Laboratories
The comparative pharmacology and up-regulation of rat neuronal nicotinic receptor subtype binding sites stably expressed in transfected mammalian cells.
J Pharmacol Exp Ther 310: 98-107 (2004)
Georgetown University
Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].
Bioorg Med Chem Lett 14: 1053-6 (2004)
Roche Palo Alto
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Bioorg Med Chem Lett 14: 1049-52 (2004)
Merck Research Laboratories
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Bioorg Med Chem Lett 14: 1043-8 (2004)
Merck Frosst Centre For Therapeutic Research
The development of potent non-peptidic PTP-1B inhibitors.
Bioorg Med Chem Lett 14: 1039-42 (2004)
Merck Frosst Centre For Therapeutic Research
1,2-Benzothiazine 1,1-dioxide alpha-ketoamide analogues as potent calpain I inhibitors.
Bioorg Med Chem Lett 14: 1035-8 (2004)
Cephalon
Benzodiazepine-based selective inhibitors of mitochondrial F1F0 ATP hydrolase.
Bioorg Med Chem Lett 14: 1031-4 (2004)
Pharmaceutical Research Institute
N-[1-Aryl-2-(1-imidazolo)ethyl]-guanidine derivatives as potent inhibitors of the bovine mitochondrial F1F0 ATP hydrolase.
Bioorg Med Chem Lett 14: 1027-30 (2004)
Pharmaceutical Research Institute
4-Substituted anilides as selective melatonin MT2 receptor agonists.
Bioorg Med Chem Lett 14: 1023-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Anti-inflammatory flavonoids and pterocarpanoid from Crotalaria pallida and C. assamica.
Bioorg Med Chem Lett 14: 1011-4 (2004)
Kaohsiung Medical University
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
Bioorg Med Chem Lett 14: 1003-5 (2004)
Virginia Commonwealth University
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.
Bioorg Med Chem Lett 14: 999-1002 (2004)
Virginia Commonwealth University
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.
Bioorg Med Chem Lett 14: 989-93 (2004)
Millennium Pharmaceuticals
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.
Bioorg Med Chem Lett 14: 983-7 (2004)
Millennium Pharmaceuticals
Synthesis and evaluation of S-4-(3-thienyl)phenyl-alpha-methylacetic acid.
Bioorg Med Chem Lett 14: 979-82 (2004)
National Institute of Pharmaceutical Education and Research
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.
Bioorg Med Chem Lett 14: 967-71 (2004)
Boehringer Ingelheim (Canada)
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorg Med Chem Lett 14: 959-63 (2004)
Glaxosmithkline
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
Bioorg Med Chem Lett 14: 953-7 (2004)
Glaxosmithkline
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Bioorg Med Chem Lett 14: 947-52 (2004)
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Bioorg Med Chem Lett 14: 941-5 (2004)
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Bioorg Med Chem Lett 14: 935-9 (2004)
Merck Research Laboratories
A new series of potent oxindole inhibitors of CDK2.
Bioorg Med Chem Lett 14: 913-7 (2004)
Hoffmann-La Roche
Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR.
Bioorg Med Chem Lett 14: 909-12 (2004)
Merck Research Laboratories
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.
Bioorg Med Chem Lett 14: 875-9 (2004)
Kirin Brewery
Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX.
Bioorg Med Chem Lett 14: 869-73 (2004)
Slovak Academy of Sciences
3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.
Bioorg Med Chem Lett 14: 865-8 (2004)
Abbott Laboratories
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 859-63 (2004)
Merck Research Laboratories
Miraziridine A: natures blueprint towards protease class-spanning inhibitors.
Bioorg Med Chem Lett 14: 855-7 (2004)
Institut FüR Biochemie
Inhibitory effects on mushroom tyrosinase by some alkylbenzaldehydes.
J Enzyme Inhib Med Chem 18: 491-6 (2003)
Xiamen University
Evaluation of indole esters as inhibitors of p60(c-Src) receptor tyrosine kinase and investigation of the inhibition using receptor docking studies.
J Enzyme Inhib Med Chem 18: 485-90 (2003)
Kobe Gakuin University
HIV protease inhibitors are inhibitors but not substrates of the human breast cancer resistance protein (BCRP/ABCG2).
J Pharmacol Exp Ther 310: 334-41 (2004)
University of Washington
Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A.
Bioorg Med Chem Lett 14: 1599-602 (2004)
Abbott Laboratories
Design, synthesis and structure-activity relationship of novel RXR-selective modulators.
Bioorg Med Chem Lett 14: 1593-8 (2004)
Ligand Pharmaceuticals
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bioorg Med Chem Lett 14: 1577-80 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological activity of selective azasugar-based TACE inhibitors.
Bioorg Med Chem Lett 14: 1569-72 (2004)
Organon K.K.
Thrombin inhibitors built on an azaphenylalanine scaffold.
Bioorg Med Chem Lett 14: 1563-7 (2004)
University of Ljubljana
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.
Bioorg Med Chem Lett 14: 1527-31 (2004)
Kyoto Pharmaceutical University
Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-alpha-induced VCAM-1 expression.
Bioorg Med Chem Lett 14: 1513-7 (2004)
Atherogenics
Structure-activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.
Bioorg Med Chem Lett 14: 1503-7 (2004)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.
Bioorg Med Chem Lett 14: 1495-8 (2004)
Inotek Pharmaceuticals
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
Bioorg Med Chem Lett 14: 1491-3 (2004)
Hoffmann-La Roche
New PDMP analogues inhibit process outgrowth in an insect cell line.
Bioorg Med Chem Lett 14: 1487-90 (2004)
University of Arizona
Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.
Bioorg Med Chem Lett 14: 1483-6 (2004)
Bristol-Myers Squibb Pharmaceuticals Research Institute
Identification of novel potent bicyclic peptide deformylase inhibitors.
Bioorg Med Chem Lett 14: 1477-81 (2004)
Genomics Institute of The Novartis Research Foundation
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists.
Bioorg Med Chem Lett 14: 1471-6 (2004)
Pfizer
Determination of the stable conformation of GABA(A)-benzodiazepine receptor bivalent ligands by low temperature NMR and X-ray analysis.
Bioorg Med Chem Lett 14: 1465-9 (2004)
University of Wisconsin-Milwaukee
Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta.
Bioorg Med Chem Lett 14: 1455-9 (2004)
Cell Therapeutics
HIV-1 integrase pharmacophore model derived from diverse classes of inhibitors.
Bioorg Med Chem Lett 14: 1447-54 (2004)
University of Houston
Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.
Bioorg Med Chem Lett 14: 1441-6 (2004)
Vertex Pharmaceuticals
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.
Bioorg Med Chem Lett 14: 1417-21 (2004)
Merck Research Laboratories
Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.
Bioorg Med Chem Lett 14: 1411-6 (2004)
Wyeth Research
Crucial amides for dimerization inhibitors of HIV-1 protease.
Bioorg Med Chem Lett 14: 1395-8 (2004)
Purdue University
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