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

D O Arnaiz¹, Z Zhao, A Liang

¹Discovery Research, Berlex Biosciences, Richmond, CA 94804, USA. damian_arnaiz@berlex.com

Bioorganic & Medicinal Chemistry Letters

|June 15, 2000

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.

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