2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists

J Med Chem. 2008 Jul 10;51(13):3946-52. doi: 10.1021/jm800199h. Epub 2008 Jun 14.

Abstract

Selective bradykinin (BK) B 1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure activity relationships of the structurally novel HTS lead compound 1 provided potent hBK B 1 receptor antagonists with excellent receptor occupancy in the CNS of hBK B 1 transgenic rats.

MeSH terms

  • Amines / chemistry*
  • Animals
  • Benzophenones / chemical synthesis
  • Benzophenones / chemistry*
  • Benzophenones / pharmacology*
  • Bradykinin B1 Receptor Antagonists*
  • Cell Line
  • Dogs
  • Humans
  • Molecular Structure
  • Rats
  • Receptor, Bradykinin B1 / metabolism
  • Structure-Activity Relationship

Substances

  • Amines
  • Benzophenones
  • Bradykinin B1 Receptor Antagonists
  • Receptor, Bradykinin B1