title: Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids.
abstract: 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.
authors.affiliation: Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France. jidong.zhang@aventis.com
authors.forename: J
authors.initials: J
authors.lastname: Zhang
authors.forename: S
authors.initials: S
authors.lastname: Didierlaurent
authors.forename: M
authors.initials: M
authors.lastname: Fortin
authors.forename: D
authors.initials: D
authors.lastname: Lefrançois
authors.forename: E
authors.initials: E
authors.lastname: Uridat
authors.forename: J P
authors.initials: JP
authors.lastname: Vevert
mesh_terms: D002264:Carboxylic Acids / Q000378:metabolism*; D016232:Endothelins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011720:Pyrazoles / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D002264:Carboxylic Acids; D016232:Endothelins; D011720:Pyrazoles