(N-ACYL-N-ALKYL)GLYCYL BOROLYSINE ANALOGS - A NEW CLASS OF POTENT THROMBIN INHIBITORS

Authors
GALEMMO RA FEVIG JM CARINI DJ CACCIOLA J WELLS BL HILLYER GL BURIAK J ROSSI KA STOUTEN PFW ALEXANDER RS HILMER R BOSTROM L ABELMAN MM LEE SL WEBER PC KETTNER CA KNABB RM WEXLER RR
Citation
Ra. Galemmo et al., (N-ACYL-N-ALKYL)GLYCYL BOROLYSINE ANALOGS - A NEW CLASS OF POTENT THROMBIN INHIBITORS, Bioorganic & medicinal chemistry letters, 6(24), 1996, pp. 2913-2918
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
24
Year of publication
1996
Pages
2913 - 2918
Database
ISI
SICI code
0960-894X(1996)6:24<2913:(BA-AN>2.0.ZU;2-T
Abstract
In this report the structure-activity relationships of a series of nov el (N-acyl-N-alkyl)glycyl borolysine thrombin inhibitors are described . This work culminates in the discovery of (N-3-phenylpropanoyl-N-phen ethyl) glycyl borolysine (12j), a potent, orally active inhibitor with a binding conformation in which the N-phenethyl group occupies the ar yl binding pocket of thrombin. Copyright (C) 1996 The DuPont Merck Pha rmaceutical Company. Published by Elsevier Science Ltd