Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.
We have previously reported the identification of pyrazole-5-carboxylic acids as a new class of endothelin antagonists from low affinity pyrazol-5-ol ligands, which were obtained by random screening assays. We describe herein the synthesis and the structure activity relationships (SARs) of these pyrazole-5-carboxylic acids with potent ET(A) selective, mixed ET(A)/ET(B) or moderately ET(B) selective antagonist activities.
Zhang
J
J
Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France. jidong.zhang@aventis.com
Didierlaurent
S
S
Fortin
M
M
Lefrançois
D
D
Uridat
E
E
Vevert
J P
JP
D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016232:Endothelins / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000737:chemistry*; D013329:Structure-Activity Relationship
D002264:Carboxylic Acids; D016232:Endothelins; D011720:Pyrazoles