Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: Transition state inhibitors

Authors
Bachand, B Tarazi, M St-Denis, Y Edmunds, JJ Winocour, PD Leblond, L Siddiqui, MA
Citation
B. Bachand et al., Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: Transition state inhibitors, BIOORG MED, 11(3), 2001, pp. 287-290
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
3
Year of publication
2001
Pages
287 - 290
Database
ISI
SICI code
0960-894X(20010212)11:3<287:PASBLI>2.0.ZU;2-1
Abstract
Bicyclic piperazinone based thrombin inhibitors of general structure 2 were prepared and evaluated in vitro and in vivo. These inhibitors, having in c ommon an electrophilic basic trans-cyclohexylamine P-1 residue, displayed h igh thrombin affinity, high selectivity against trypsin and good in vivo ef ficacy in the rat arterial thrombosis model. (C) 2001 Elsevier Science Ltd. All rights reserved.