PMID

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Article Title

Organization

Chemical synthesis of tetracyclic terpenes and evaluation of antagonistic activity on endothelin-A receptors and voltage-gated calcium channels.

Kansas State University

Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity.

Southeast University

New chlorinated diphenyl ethers from an Aspergillus species.

University of Western Australia

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

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

Endothelin: a new challenge.

Warner-Lambert

Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.

Merck

 

Structure-activity relationships of monocyclic endothelin analogs

TBA

 

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

TBA

 

Pyridazinones with a pendant acylsulfonamide moiety as endothelin receptor antagonists

TBA

 

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

TBA

 

Quantitative structure-activity relationships study of endothelin-1 analogs

TBA

 

Structure-activity relationships in a series of monocyclic endothelin analogues

TBA

Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.

University of Innsbruck

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

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

Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.

Hoechst Marion Roussel

Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.

Shionogi

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

From bosentan (TracleerŪ) to macitentan (OpsumitŪ): The medicinal chemistry perspective.

Actelion Pharmaceuticals

Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives.

RhôNe-Poulenc Rorer

Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.

Merck

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

Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.

RhôNe-Poulenc Rorer

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.

Abbott Laboratories

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

Azole endothelin antagonists. 2. Structure-activity studies.

Abbott Laboratories

Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.

Abbott Laboratories

The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.

Bristol-Myers Squibb Pharmaceutical Research Institute

Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute