111 articles for thisTarget
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Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Metabolism study and biological evaluation of bosentan derivatives.
University of Perugia
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity.
Southeast University
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.
Actelion Pharmaceuticals
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.
Encysive Pharmaceuticals
Selective optimization of side activities: another way for drug discovery.
Prestwick Chemical
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Tanabe Seiyaku
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).
Bristol-Myers Squibb Pharmaceutical Research Institute
Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.
Rh£Ne-Poulenc Rorer
Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.
Warner-Lambert
Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.
Tsukuba Research Institute
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
Takeda Chemical Industries
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.
Warner-Lambert
Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications.
TBA
Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.
Merck
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan
TBA
Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptide
TBA
Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity
TBA
Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography.
University Hospital Mu£Nster
Synthesis and pharmacological activity of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acids as selective ET(A) antagonists.
St. John'S University
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
PET-compatible endothelin receptor radioligands: synthesis and first in vitro and in vivo studies.
University Hospital M£Nster
A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruri
TBA
Search for surrogates: A study of endothelin receptor antagonist structure activity relationships
TBA
γ-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs
TBA
2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonists
TBA
Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists
TBA
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
TBA
Discovery of substituted 8,9-dicarboxyldibenzo [2,3:5,6] bicyclo [5.2.0] nonan-4-ones with moderate binding affinity to the endothelin ETA and ETB receptors
TBA
Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III)
TBA
Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[16–21, D-His16]
TBA
Targeted Drugs for Treatment of Pulmonary Arterial Hypertension: Past, Present, and Future Perspectives.
Shanghai Institute of Materia Medica
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.
Covx Research
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Actelion Pharmaceuticals
Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.
University of Innsbruck
Structure-activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.
Actelion Pharmaceuticals
Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.
Tsukuba Research Institute
Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships of a novel class of endothelin-A receptor antagonists and discovery of potent and selective receptor antagonist, 2-(benzo[1,3]dioxol-5-yl)-6-isopropyloxy-4-(4-methoxyphenyl)-2H-chromene-3-carboxylic acid (S-1255). 1. Study on structure-activity relationships and bas
Shionogi
Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.
Bristol-Myers Squibb Pharmaceutical Research Institute
The design and synthesis of a novel series of indole derived selective ET(A) antagonists.
Pfizer
Modifications and structure-activity relationships at the 2-position of 4-sulfonamidopyrimidine derivatives as potent endothelin antagonists.
Tanabe Seiyaku
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.
Abbott Laboratories
Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Tanabe Seiyaku
Isoindolines: a new series of potent and selective endothelin-A receptor antagonists.
Novartis Institute For Biomedical Research
Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.
Hoechst Marion Roussel
Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Endothelin-Receptor Antagonists beyond Pulmonary Arterial Hypertension: Cancer and Fibrosis.
Centre Hospitalier Universitaire Vaudois (Chuv)
Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids.
Hoechst Marion Roussel
Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.
Iowa State University
From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
Actelion Pharmaceuticals
Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.
Abbott Laboratories
Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist.
Basf
Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.
Merck
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630.
Takarazuka Research Institute
Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.
Takarazuka Research Institute
Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.
Merck
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.
Abbott Laboratories
Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.
Immunopharmaceutics
Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.
Immunopharmaceutics
Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.
Warner-Lambert
Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.
Abbott Laboratories
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Abbott Laboratories
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
Basf
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
Abbott Laboratories
Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.
Abbott Laboratories
1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.
Smithkline Beecham Pharmaceuticals
Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists.
Warner-Lambert
Structure-activity relationships of the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists.
Warner-Lambert
Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists.
Tsukuba Research Institute
Design, synthesis and evaluation of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives as ET
St. John'S University
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs.
Queen'S University
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Johnson & Johnson Pharmaceutical