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

Bioorg Med Chem Lett. 2000 Nov 20;10(22):2575-8. doi: 10.1016/s0960-894x(00)00513-8.

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.

MeSH terms

  • Carboxylic Acids / chemical synthesis*
  • Carboxylic Acids / chemistry
  • Carboxylic Acids / pharmacology
  • Endothelins / antagonists & inhibitors*
  • Pyrazoles / chemistry*
  • Structure-Activity Relationship

Substances

  • Carboxylic Acids
  • Endothelins
  • Pyrazoles