PMID

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Article Title

Organization

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

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

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

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

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

Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications.

TBA

 

Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan

TBA

 

Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity

TBA

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

 

A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruri

TBA

 

Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists

TBA

 

Search for surrogates: A study of endothelin receptor antagonist structure activity relationships

TBA

 

γ-Carbamate butenolide analogues as potent ET_A selective endothelin receptor antagonists and prodrugs

TBA

 

2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and et_A selective endothelin receptor antagonists

TBA

 

1,4-Diaryl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acids as endothelin receptor antagonists

TBA

 

1,3-diaryl-2-carboxyindoles as potent non-peptide endothelin antagonists

TBA

 

Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists

TBA

 

Thiophenesulfonamides as endothelin receptor antagonists

TBA

 

Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists

TBA

 

1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists

TBA

 

Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptors

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 ET_A and ET_B receptors

TBA

 

Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III)

TBA

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

Solid-phase synthesis of endothelin receptor antagonists.

Basf

The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.

Actelion Pharmaceuticals

Bis-sulfonamides 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

Pyridine alkaloids with activity in the central nervous system.

University of Auckland

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

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)

Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.

Iowa State University

From bosentan (TracleerŪ) to macitentan (OpsumitŪ): 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

Butenolide endothelin antagonists with improved aqueous solubility.

Warner-Lambert

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

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

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

Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.

Yogi Vemana University

Syntheses, cholinesterases inhibition, and molecular docking studies of pyrido[2,3-b]pyrazine derivatives.

University of Karachi

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.

University of Leipzig