Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors

Bioorg Med Chem Lett. 2000 May 1;10(9):957-61. doi: 10.1016/s0960-894x(00)00138-4.

Abstract

A series of indole and carbazole based inhibitors of factor Xa (FXa) has been investigated. The most potent compound inhibits FXa with a Ki of 0.2 nM and has 900- and 750-fold selectivity over thrombin and trypsin, respectively.

MeSH terms

  • Amidines / chemistry*
  • Anticoagulants / chemical synthesis*
  • Anticoagulants / pharmacology*
  • Carbazoles / chemical synthesis*
  • Carbazoles / chemistry
  • Carbazoles / pharmacology*
  • Chemical Phenomena
  • Chemistry, Physical
  • Crystallography, X-Ray
  • Factor Xa Inhibitors*
  • Humans
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Models, Molecular
  • Molecular Conformation
  • Pyridines / chemistry*
  • Structure-Activity Relationship
  • Thrombin / antagonists & inhibitors
  • Trypsin Inhibitors / chemical synthesis
  • Trypsin Inhibitors / pharmacology

Substances

  • Amidines
  • Anticoagulants
  • Carbazoles
  • Factor Xa Inhibitors
  • Indoles
  • Pyridines
  • Trypsin Inhibitors
  • Fidexaban
  • Thrombin

Associated data

  • PDB/1QB9