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

Authors
Arnaiz, DO Zhao, ZS Liang, A Trinh, L Whitlow, M Koovakkat, SK Shaw, KJ
Citation
Do. Arnaiz et al., Design, synthesis, and in vitro biological activity of indole-based factorXa inhibitors, BIOORG MED, 10(9), 2000, pp. 957-961
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
9
Year of publication
2000
Pages
957 - 961
Database
ISI
SICI code
0960-894X(20000501)10:9<957:DSAIVB>2.0.ZU;2-#
Abstract
A series of indole and carbazole based inhibitors of factor Xa (FXa) has be en 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, respectiv ely. (C) 2000 Elsevier Science Ltd. All rights reserved.