1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: A novel series of thrombin inhibitors

Authors
Takeuchi, K Bastian, JA Gifford-Moore, DS Harper, RW Miller, SC Mullaney, JT Sall, DJ Smith, GF Zhang, MS Fisher, MJ
Citation
K. Takeuchi et al., 1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: A novel series of thrombin inhibitors, BIOORG MED, 10(20), 2000, pp. 2347-2351
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2347 - 2351
Database
ISI
SICI code
0960-894X(20001016)10:20<2347:1IAABD>2.0.ZU;2-B
Abstract
A novel series of 1,2-disubstituted indole, azaindole and benzimidazole der ivatives possessing an amine moiety was identified as thrombin inhibitors. An indole with basic diamine moieties (12a) was the most potent thrombin in hibitor in the series with K-ass = 197 x 10(6) L/mol. (C) 2000 Elsevier Sci ence Ltd. All rights reserved.