The discovery of orally available thrombin inhibitors: Optimisation of theP1 pharmacophore

Authors
Ambler, J Bentley, D Brown, L Dunnet, K Farr, D Janus, D Le Grand, D Menear, K Mercer, M Talbot, M Tweed, M Wathey, B
Citation
J. Ambler et al., The discovery of orally available thrombin inhibitors: Optimisation of theP1 pharmacophore, BIOORG MED, 9(8), 1999, pp. 1103-1108
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
8
Year of publication
1999
Pages
1103 - 1108
Database
ISI
SICI code
0960-894X(19990419)9:8<1103:TDOOAT>2.0.ZU;2-8
Abstract
Thrombin inhibitors have been designed with the replacement of the strongly basic guanidine P1 pharmocophore with a group that exploits the lipophilic ty of the S1 pocket. The approach has lead to the discovery of potent throm bin inhibitors demonstrating good intra-duodenal absorption. (C) 1999 Elsev ier Science Ltd. All rights reserved.