The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold

Bioorg Med Chem Lett. 1999 Feb 8;9(3):463-8. doi: 10.1016/s0960-894x(99)00015-3.

Abstract

The Bradykinin B2 receptor antagonist HOE 140 (D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg) has been used as a template for the de novo design and synthesis of a small number of non-peptide lead compounds based on the 1,4-benzodiazepin-2-one framework. Two of the compounds have been found to exhibit moderate K(i) values of 8.9 and 9.2 microM at the human Bradykinin B2 receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bradykinin / analogs & derivatives*
  • Bradykinin / chemistry
  • Bradykinin / pharmacology
  • Bradykinin Receptor Antagonists*
  • Drug Design
  • Humans
  • Molecular Mimicry*
  • Receptor, Bradykinin B2

Substances

  • Bradykinin Receptor Antagonists
  • Receptor, Bradykinin B2
  • icatibant
  • Bradykinin