Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids |
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Authors: | Zhang J Didierlaurent S Fortin M Lefrançois D Uridat E Vevert J P |
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Institution: | Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France. jidong.zhang@aventis.com |
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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. |
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