Design, Synthesis, And In Vitro Biological Activity Of Indole-Based Factor Xa Inhibitors

A series of indole and carbazole based inhibitors of factor Xa (FXa) has been investigated. The most potent compound inhibits FXa with a K-i of 0.2 nM and has 900- and 750-fold selectivity over thrombin and trypsin, respectively. (C) 2000 Elsevier Science Ltd. All rights reserved.