Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications

Authors
Plummer, JS Berryman, KA Cai, C Cody, WL DiMaio, J Doherty, AM Edmunds, JJ He, JX Holland, DR Levesque, S Kent, DR Narasimhan, LS Rubin, JR Rapundalo, ST Siddiqui, MA Susser, AJ St-Denis, Y Winocour, PD
Citation
Js. Plummer et al., Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications, BIOORG MED, 8(23), 1998, pp. 3409-3414
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
23
Year of publication
1998
Pages
3409 - 3414
Database
ISI
SICI code
0960-894X(199812)8:23<3409:PASBLI>2.0.ZU;2-N
Abstract
The synthesis and antithrombotic activity of a series of nonpeptide bicycli c thrombin inhibitors is described. We have explored the SAR with modificat ions to the pi site. The introduction of arginine mimetics at the pi site l ed to potent and selective thrombin inhibitors. (C) 1998 Elsevier Science L td. All rights reserved.