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ID: ALA1133200

Journal: Bioorg Med Chem Lett

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

Authors: Zhang J, Didierlaurent S, Fortin M, Lefrançois D, Uridat E, Vevert JP.

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.

CiteXplore: 10890162

DOI: 10.1016/s0960-894x(00)00232-8