Literature DB >> 10890162

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

J Zhang1, S Didierlaurent, M Fortin, D Lefrançois, E Uridat, J P Vevert.   

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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Year:  2000        PMID: 10890162     DOI: 10.1016/s0960-894x(00)00232-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

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Authors:  Xiangbo Zhao; David W C MacMillan
Journal:  J Am Chem Soc       Date:  2020-11-09       Impact factor: 15.419

2.  Michael-type addition of azoles of broad-scale acidity to methyl acrylate.

Authors:  Sławomir Boncel; Kinga Saletra; Barbara Hefczyc; Krzysztof Z Walczak
Journal:  Beilstein J Org Chem       Date:  2011-02-08       Impact factor: 2.883

  2 in total

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