Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors

J Med Chem. 2008 Jun 12;51(11):3077-80. doi: 10.1021/jm8002697. Epub 2008 May 7.

Abstract

Recently, FXIIa was highlighted as an original attractive target for the development of new anticoagulant drugs with low rates of therapy-related hemorrhages. In this work, we describe the development of a new series of 3-carboxamide-coumarins that are the first potent and selective nonpeptidic inhibitors of FXIIa.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Anticoagulants / chemical synthesis*
  • Anticoagulants / chemistry
  • Coumarins / chemical synthesis*
  • Coumarins / chemistry
  • Factor XIIa / antagonists & inhibitors*
  • Factor XIIa / chemistry
  • Structure-Activity Relationship

Substances

  • Amides
  • Anticoagulants
  • Coumarins
  • Factor XIIa