Neutral inhibitors of the serine protease factor Xa

Authors
Shrader, WD Young, WB Sprengeler, PA Sangalang, JC Elrod, K Carr, G
Citation
Wd. Shrader et al., Neutral inhibitors of the serine protease factor Xa, BIOORG MED, 11(14), 2001, pp. 1801-1804
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
14
Year of publication
2001
Pages
1801 - 1804
Database
ISI
SICI code
0960-894X(20010723)11:14<1801:NIOTSP>2.0.ZU;2-2
Abstract
A neutral inhibitor of the serine protease factor Xa was identified via a h igh throughput screen of a commercial library. The initial lead 1 demonstra ted reversible and competitive inhibition kinetics for factor Xa and posses sed a high degree of selectivity versus other related serine proteases. Ini tial modeling efforts and the generation of a series of analogues of 1 are described. (C) 2001 Elsevier Science Ltd. All rights reserved.