Literature DB >> 11086733

Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.

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

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.

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Year:  2000        PMID: 11086733     DOI: 10.1016/s0960-894x(00)00513-8

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


  2 in total

1.  Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair.

Authors:  Monika I Antczak; Yongyou Zhang; Changguang Wang; Jennifer Doran; Jacinth Naidoo; Sukesh Voruganti; Noelle S Williams; Sanford D Markowitz; Joseph M Ready
Journal:  J Med Chem       Date:  2017-04-25       Impact factor: 7.446

2.  Synthesis of tetrasubstituted pyrazoles containing pyridinyl substituents.

Authors:  Josef Jansa; Ramona Schmidt; Ashenafi Damtew Mamuye; Laura Castoldi; Alexander Roller; Vittorio Pace; Wolfgang Holzer
Journal:  Beilstein J Org Chem       Date:  2017-05-12       Impact factor: 2.883

  2 in total

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