Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications

Authors
St-Denis, Y Augelli-Szafran, CE Bachand, B Berryman, KA DiMaio, J Doherty, AM Edmunds, JJ Leblond, L Levesque, S Narasimhan, LS Penvose-Yi, JR Rubin, JR Tarazi, M Winocour, PD Siddiqui, MA
Citation
Y. St-denis et al., Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications, BIOORG MED, 8(22), 1998, pp. 3193-3198
Citations number
10
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
22
Year of publication
1998
Pages
3193 - 3198
Database
ISI
SICI code
0960-894X(19981117)8:22<3193:PBLIOT>2.0.ZU;2-K
Abstract
Peptidomimetic inhibitors of general structure 1 have been prepared. Optimi zation of the binding affinities of these compounds through variation of th e P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting pharmacological profiles both in vitro and in vivo. (C) 1998 Elsevier Science Ltd. All rights reserved.