1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B(1) receptor antagonists

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5027-31. doi: 10.1016/j.bmcl.2008.08.014. Epub 2008 Aug 9.

Abstract

The design, synthesis, and structure-activity studies of a novel series of BK B(1) receptor antagonists based on a 1-benzylbenzimidazole chemotype are described. A number of compounds, for example, 38g, with excellent affinity for the cynomolgus macaque and rat bradykinin B(1) receptor were discovered.

MeSH terms

  • Animals
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Bradykinin B1 Receptor Antagonists*
  • Combinatorial Chemistry Techniques
  • Dogs
  • Drug Design
  • Molecular Structure
  • Rats
  • Structure-Activity Relationship

Substances

  • Benzimidazoles
  • Bradykinin B1 Receptor Antagonists