Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids

Random screening of compounds in endothelin receptor (ET A and ET B) binding assays led to the discovery of a new class of pyrazol-5-ol ligands. Characterization of structural features crucial for binding activities of these pyrazol-5-ols, by structure–activity-relationship (SAR) studies, allowed us...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-06, Vol.10 (12), p.1351-1355
Hauptverfasser:	Zhang, Jidong, Didierlaurent, Stanislas, Fortin, Michel, Lefrançois, Dominique, Uridat, Eric, Vevert, Jean Paul
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Carboxylic Acids - metabolism Cardiovascular system Endothelins - antagonists & inhibitors Endothelins - metabolism Medical sciences Pharmacology. Drug treatments Pyrazoles - metabolism Structure-Activity Relationship Vasodilator agents. Cerebral vasodilators
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Beschreibung
Zusammenfassung:	Random screening of compounds in endothelin receptor (ET A and ET B) binding assays led to the discovery of a new class of pyrazol-5-ol ligands. Characterization of structural features crucial for binding activities of these pyrazol-5-ols, by structure–activity-relationship (SAR) studies, allowed us to design a novel class of pyrazole-5-carboxylic acids as more potent ET antagonists.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00232-8