PMID

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Article Title

Organization

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

Southeast University

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

Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.

Warner-Lambert

Endothelin: a new challenge.

Warner-Lambert

Design of a functional hexapeptide antagonist of endothelin.

Warner-Lambert

 

Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelin

TBA

 

Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptide

TBA

 

Quantitative structure-activity relationships study of endothelin-1 analogs

TBA

 

Structure-activity relationships in a series of monocyclic endothelin analogues

TBA

 

Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[16–21, D-His¹⁶]

TBA

 

CGS 27830, a potent nonpeptide endothelin receptor antagonist

TBA

Modifications and structure-activity relationships at the 2-position of 4-sulfonamidopyrimidine derivatives as potent endothelin antagonists.

Tanabe Seiyaku

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

Hoechst Marion Roussel

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

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

N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.

Pudue Pharma Discovery Research

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories