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Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic
J Zhang1, S Didierlaurent, M Fortin
1Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France. jidong.zhang@aventis.com
Bioorganic & Medicinal Chemistry Letters
|November 22, 2000
Abstract:
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.