Citation
K. Lee et al., Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption, BIOORG MED, 9(17), 1999, pp. 2483-2486
Citations number
25
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X
→ ACNP
Volume
9
Issue
17
Year of publication
1999
Pages
2483 - 2486
Database
ISI
SICI code
0960-894X(19990906)9:17<2483:FTIIOF>2.0.ZU;2-7
Abstract
LB30057 (1) is a selective and efficacious oral thrombin inhibitor. Fluorin
e-substitution on the phenylene ring of the benzamidrazone portion in both
compound 1 and its derivatives gave, in many cases, enhanced oral absorptio
n in rats while maintaining the intrinsic potency and selectivity. Compound
2 demonstrated a 3-fold increase in absorption. (C) 1999 Elsevier Science
Ltd. All rights reserved.