Bicyclic pyridones as potent, efficacious and orally bioavailable thrombininhibitors

Authors
Coburn, CA Rush, DM Williams, PD Homnick, C Lyle, EA Lewis, SD Lucas, BJ Di Muzio-Mower, JM Juliano, M Krueger, JA Vastag, K Chen, IW Vacca, JP
Citation
Ca. Coburn et al., Bicyclic pyridones as potent, efficacious and orally bioavailable thrombininhibitors, BIOORG MED, 10(10), 2000, pp. 1069-1072
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
10
Year of publication
2000
Pages
1069 - 1072
Database
ISI
SICI code
0960-894X(20000515)10:10<1069:BPAPEA>2.0.ZU;2-3
Abstract
A new class of conformationally constrained thrombin inhibitors is describe d. These compounds contain a unique bicyclic pyridone scaffold which serves as a P3P2 dipeptide surrogate. The synthesis and antithrombotic activity o f these inhibitors is reported. (C) 2000 Elsevier Science Ltd. All rights r eserved.