298 articles for thisTarget
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Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents.
Institute of Materia Medica
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.
East China University of Science and Technology
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Merck Research Laboratories
The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.
Merck Research Laboratories
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Merck Research Laboratories
Applications of Fluorine in Medicinal Chemistry.
Bristol-Myers Squibb Research and Development
Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes.
National Institute of Pharmaceutical Education and Research-Ahmedabad
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.
Glaxosmithkline
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.
Xuanzhu Pharma
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
Shanghai Institute of Materia Medica
Design, Synthesis, and Pharmacological Evaluation of Fusedß-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.
Chinese Academy of Sciences
Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold.
University Park Nottingham
Synthesis and potent inhibitory activities of carboxybenzyl-substituted 8-(3-(R)-aminopiperidin-1-yl)-7-(2-chloro/cyanobenzyl)-3-methyl-3,7-dihydro-purine-2,6-diones as dipeptidyl peptidase IV (DPP-IV) inhibitors.
Southern Medical University
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors: use of a carboxylate prodrug to improve bioavailability.
Sumitomo Dainippon Pharma
Structure based virtual screening of MDPI database: discovery of structurally diverse and novel DPP-IV inhibitors.
Jamia Hamdard
(R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: design, synthesis, biological evaluation, and molecular modeling.
Chinese Academy of Sciences
Thiophenes, polyacetylenes and terpenes from the aerial parts of Eclipata prostrate.
TBA
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP).
University of Antwerp
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?
Chuv-Unil
Design, synthesis and biological evaluation of novel aminomethyl-piperidones based DPP-IV inhibitors.
M.S. University of Baroda
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Merck
A general method for making peptide therapeutics resistant to serine protease degradation: application to dipeptidyl peptidase IV substrates.
Tufts University
Integrated Synthesis and Testing of Substituted Xanthine Based DPP4 Inhibitors: Application to Drug Discovery.
Sanofi-Aventis
Discovery of potent dipeptidyl peptidase IV inhibitors through pharmacophore hybridization and hit-to-lead optimization.
Chinese Academy of Science
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.
Tufts University Sackler School of Biomedical Sciences
Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors.
Bristol-Myers Squibb Research and Development
Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors.
Toray Industries
P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy.
University of Antwerp
Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors.
Takeda California
Remarkable potential of thea-aminophosphonate/phosphinate structural motif in medicinal chemistry.
Wroclaw University of Technology
Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Mitsubishi Tanabe Pharma
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.
Dainippon Sumitomo Pharma
Dipeptidyl peptidase-4 inhibitor withß-amino amide scaffold: synthesis, SAR and biological evaluation.
Dong-A Pharm.
4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities.
Tufts University School of Medicine
Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group.
Mitsubishi Tanabe Pharma
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.
University of Antwerp (Ua)
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.
Chinese Academy of Sciences
An example of designed multiple ligands spanning protein classes: dual MCH-1R antagonists/DPPIV inhibitors.
Prosidion
Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554.
Takeda Pharmaceutical
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor.
Takeda Pharmaceutical
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.
Chinese Academy of Sciences
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
National Health Research Institutes
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.
Mcgill University
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.
Sichuan University
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.
Matrix Laboratories
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.
Taisho Pharmaceutical
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
Boehringer Ingelheim Pharma
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.
Takeda California
Discovery of long-acting N-(cyanomethyl)-N-alkyl-L-prolinamide inhibitors of dipeptidyl peptidase IV.
Minase Research Institute
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group.
Ono Pharmaceutical
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.
Merck Research Laboratories
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
Merck Research Laboratories
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors.
Korea Research Institute of Chemical Technology
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Pfizer
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors.
Mitsubishi Pharma
Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.
Korea Research Institute of Chemical Technology
Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.
Korea Research Institute of Chemical Technology
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.
Pharmaceutical Research Institute
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.
University of Antwerp (Uia)
Specific and irreversible cyclopeptide inhibitors of dipeptidyl peptidase IV activity of the T-cell activation antigen CD26.
University of Versailles Saint-Quentin-en-Yvelines
Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.
Boehringer Ingelheim Pharmaceuticals
Development of potent and selective dipeptidyl peptidase II inhibitors.
University of Antwerp (Uia)
1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors.
Novartis Institute For Biomedical Research
Nonpeptide small-molecular inhibitors of dipeptidyl peptidase IV: N-phenylphthalimide analogs.
University of Tokyo
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.
Argenta Discovery
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.
Sanwa Kagaku Kenkyusho
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.
Bristol-Myers Squibb Research and Development
Molecular dynamics simulations and MM/GBSA methods to investigate binding mechanisms of aminomethylpyrimidine inhibitors with DPP-IV.
Graduate University of The Chinese Academy of Sciences
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.
Dainippon Sumitomo Pharma
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
University of Antwerp (Ua)
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554.
Takeda Pharmaceutical
Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.
Dong-A Pharm.
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-relateda-glucosidase inhibitors and liver X receptor antagonists.
The University of Tokyo
Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases.
Tufts University Sackler School of Graduate Biomedical Sciences
Aza-annulation on the 16-dehydropregnenolone, via tandem intermolecular aldol process and intramolecular Michael addition.
Central Drug Research Institute
Design, Synthesis, and in Vitro Evaluation of Novel Aminomethyl-pyridines as DPP-4 Inhibitors.
TBA
Discovery of potent dipeptidyl peptidase IV inhibitors derived fromß-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes.
Shandong University of Traditional Chinese Medicine
1-((3S,4S)-4-amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes.
Pfizer
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.
Merck Research Laboratories
Discovery ofß-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors.
Korea Research Institute of Chemical Technology
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.
Takeda California
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125.
Takeda Pharmaceutical
Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.
Dainippon Sumitomo Pharma
Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors.
East China University of Science and Technology
Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors.
Bristol-Myers Squibb Research and Development
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
Bristol-Myers Squibb
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.
Bristol-Myers Squibb
Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Shanghai Hengrui Pharmaceuticals
Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Shanghai Hengrui Pharmaceuticals
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
National Health Research Institutes
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor.
Torrent Pharmaceuticals
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors.
F. Hoffmann-La Roche
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
F. Hoffmann-La Roche
Application of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to different amine-containing drugs.
Instituto De Qu£Mica M£Dica (Csic)
The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements.
Santhera Pharmaceuticals (Switzerland)
From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV.
Santhera Pharmaceuticals (Switzerland)
Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV.
Santhera Pharmaceuticals (Switzerland)
Piperidinyl-2-phenethylamino inhibitors of DPP-IV for the treatment of type 2 diabetes.
Pfizer
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.
Pfizer
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
National Health Research Institutes
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.
National Health Research Institutes
Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.
Korea Research Institute of Chemical Technology
(3R)-3-amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Toray Industries
Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.
Tufts University
Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor.
Institut De Recerca BiomèDica De Barcelona
Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors.
Ranbaxy Research Laboratories
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
University of Antwerp
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors.
University of Antwerp
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.
Merck Research Laboratories
Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors.
Korea Research Institute of Chemical Technology
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors.
National Health Research Institutes
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.
Boehringer Ingelheim Pharma
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors.
Pfizer
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.
University of Antwerp
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
Bristol-Myers Squibb Research and Development
Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.
Chinese Academy of Sciences
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.
Merck Research Laboratories
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
Merck Research Laboratories
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones.
Lg Life Sciences
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.
Merck Research Laboratories
Highly Selective Inhibitors of Dipeptidyl Peptidase 9 (DPP9) Derived from the Clinically Used DPP4-Inhibitor Vildagliptin.
University of Antwerp
Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants.
Sichuan Normal University
Licochalcone A Derivatives as Selective Dipeptidyl Peptidase 4 Inhibitors with Anti-Inflammatory Effects.
Shanghai University of Traditional Chinese Medicine
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).
Merck Research Laboratories
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Merck Research Laboratories
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
F. Hoffmann-La Roche
Design and exploration of gut-restricted bifunctional molecule with TGR5 agonistic and DPP4 inhibitory effects for treating ulcerative colitis.
Shanghai Institute of Materia Medica
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors.
Mitsubishi Pharma
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration.
Minase Research Institute
Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV.
Minase Research Institute
Discovery of imeglimin-inspired novel 1,3,5-triazine derivatives as antidiabetic agents in streptozotocin-induced diabetes in Wistar rats
Sam Higginbottom University of Agriculture
Mechanistic Insight of Synthesized 1,4-Dihydropyridines as an Antidiabetic Sword against Reactive Oxygen Species.
Tanta University
3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes.
National Health Research Institutes
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.
Genentech
A review upon medicinal perspective and designing rationale of DPP-4 inhibitors.
Pcte Group of Institutes
Geminal Diheteroatomic Motifs: Some Applications of Acetals, Ketals, and Their Sulfur and Nitrogen Homologues in Medicinal Chemistry and Drug Design.
Bristol Myers Squibb Research and Early Development
Pyrrole: An insight into recent pharmacological advances with structure activity relationship.
Jamia Hamdard
Current anti-diabetic agents and their molecular targets: A review.
University of Kwazulu-Natal
Pyrazolotriazines: Biological activities, synthetic strategies and recent developments.
Mazandaran University of Medical Sciences
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.
Tufts University School of Medicine
Therapeutic potential of uracil and its derivatives in countering pathogenic and physiological disorders.
Pondicherry University
Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines.
Laboratory of Medicinal Chemistry University of Antwerp
Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.
Guru Nanak Dev University
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
Panjab University
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization.
Pfizer
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
Tianjin University
Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.
Mcgill University
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.
Glaxosmithkline
New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors.
Pfizer
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Activx Biosciences
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.
Activx Biosciences
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
National Health Research Institutes
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.
Mitsubishi Pharma
Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101.
University of Milan
Boron-Containing heterocycles as promising pharmacological agents.
Long Island University
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors.
Merck
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
Merck Research Laboratories
Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors.
University of Antwerp
Structure-activity relationship and biochemical evaluation of novel fibroblast activation protein and prolyl endopeptidase inhibitors with α-ketoamide warheads.
The Czech Academy of Sciences
Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.
Sichuan Normal University
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Galapagos
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
Novartis Institute For Biomedical Research
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.
Sungkyunkwan University
Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors.
Shanghai Jiao Tong University
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
TBA
Synthesis, in vitro evaluation, and computational simulations studies of 1,2,3-triazole analogues as DPP-4 inhibitors.
Kangwon National University
The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119.
Chinese Academy of Medical Sciences&Peking Union Medical College
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Haisco Pharmaceutical Group
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes.
East China University of Science and Technology
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.
Boehringer Ingelheim Pharma
Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors.
Merck Research Laboratories
Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors.
Guangxi Medical University
Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors.
University of Antwerp (Uia)
Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.
Government Arts College
Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study.
Guangxi Medical University
Discovery, synthesis, and in vitro evaluation of a novel bioactive peptide for ACE and DPP-IV inhibitory activity.
University of Mysore
Discovery of Highly Polar β-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors.
University of Chinese Academy of Sciences
Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.
Mcgill University
Synthesis, nitric oxide release, and dipeptidyl peptidase-4 inhibition of sitagliptin derivatives as new multifunctional antidiabetic agents.
Xi'An Jiaotong University
Nitrothiadiazolo[3,2-a]pyrimidines as promising antiglycating agents.
Ural Federal University Named After The First President of Russia B.N. Eltsin
Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin.
China Pharmaceutical University
First synthesis and determination of the absolute configuration of sulphostin, a novel inhibitor of dipeptidyl peptidase IV.
Microbial Chemistry Research Center
Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.
Tufts University School of Medicine
Novel potent nonpeptide aminopeptidase N inhibitors with a cyclic imide skeleton.
University of Tokyo
Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus.
Siberian Branch of The Russian Academy of Sciences
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.
Chinese Academy of Sciences
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.
Shanghai Jiao Tong University
Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation.
The First Affiliated Hospital of Guangzhou Medical University
Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
University of Warwick
Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors.
Chinese Academy of Sciences
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinaseδ (PI3Kδ) Inhibitors.
University Park Nottingham
Design of potent dipeptidyl peptidase IV (DPP-4) inhibitors by employing a strategy to form a salt bridge with Lys554.
Takeda Pharmaceutical
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
Ranbaxy Laboratories
N-SUBSTITUTED INDOLE DERIVATIVES AS SEROTONERGIC AGENTS USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Mindset Pharma
PREPARATION OF PHENETHYLAMINES AND CATHINONES AND STEREOISOMERS THEREOF AND PRECURSORS THEREOF
Transcend Therapeutics
Agent enhancing antitumor effect using pyrazolo[3,4-d]pyrimidine compound
Taiho Pharmaceutical
Antibacterial agents: arylalkylcarboxamido phloroglucinols
The State University of New Jersey
Kinase inhibitor compounds and compositions and methods of use
Icahn School of Medicine At Mount Sinai
2-oxo-1,2-dihydropyridine-3-carboxamide compounds and their use as inhibitors of PDK1
International Society For Drug Development
1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
Novartis
Substituted [1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists
Ogeda
Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
Saint Louis University
Ethyl N-boc piperidinyl pyrazolo pyridones as Janus kinase inhibitors
Merck Sharp & Dohme
Tetrahydronaphthyridine derivatives as mGluR2-negative allosteric modulators, compositions, and their use
TBA
Iminothiadiazine dioxides bearing an amine-linked substituent as BACE inhibitors, compositions, and their use
TBA
Green synthesis, inhibition studies of yeast a-glucosidase and molecular docking of pyrazolylpyridazine amines.
University of The Punjab
Structural and Functional Analysis of the Allosteric Inhibition of IRE1a with ATP-Competitive Ligands.
University of Washington
Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking.
China Pharmaceutical University
NAD+-dependent DNA ligase (Rv3014c) from M. tuberculosis: Strategies for inhibitor design
Central Drug Research Institute
Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687).
Schering-Plough Research Institute
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
Smithkline Beecham Pharmaceuticals
Unsaturated phosphinic analogues of gamma-aminobutyric acid as GABA(C) receptor antagonists.
University of Sydney
RP 73870, a gastrin/cholecystokinin-B receptor antagonist with potent anti-ulcer activity in the rat.
Rhone-Poulenc Rorer Central Research
Comparison of A1 adenosine receptors in brain from different species by radioligand binding and photoaffinity labelling.
UniversitÄT Heidelberg
Synthesis of unnatural flavonoids and stilbenes by exploiting the plant biosynthetic pathway in Escherichia coli.
University of Tokyo
G protein-coupled receptor kinase 2 inhibitors and methods for use of the same
The Regents of The University of Michigan
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.
Wyeth-Ayerst Research
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).
Bristol-Myers Squibb
Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).
University of Auckland
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors.
Parke-Davis Pharmaceutical Research
Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.
University of Auckland
Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.
University of Auckland
Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor
Parke-Davis Pharmaceutical Research
Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor.
University of Auckland
Increasing the cellular PKC inhibitory activity of balanol: a study of ester analogs.
Sphinx Pharmaceuticals