RATIONAL DESIGN OF BOROPEPTIDE THROMBIN INHIBITORS - BETA,BETA-DIALKYLPHENETHYLGLYCINE P2 ANALOGS OF DUP-714 WITH GREATER SELECTIVITY OVER COMPLEMENT FACTOR-I AND AN IMPROVED SAFETY PROFILE

Authors
FEVIG JM BURIAK J CACCIOLA J ALEXANDER RS KETTNER CA KNABB RM PRUITT JR WEBER PC WEXLER RR
Citation
Jm. Fevig et al., RATIONAL DESIGN OF BOROPEPTIDE THROMBIN INHIBITORS - BETA,BETA-DIALKYLPHENETHYLGLYCINE P2 ANALOGS OF DUP-714 WITH GREATER SELECTIVITY OVER COMPLEMENT FACTOR-I AND AN IMPROVED SAFETY PROFILE, Bioorganic & medicinal chemistry letters, 8(3), 1998, pp. 301-306
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
3
Year of publication
1998
Pages
301 - 306
Database
ISI
SICI code
0960-894X(1998)8:3<301:RDOBTI>2.0.ZU;2-4
Abstract
The potent boropeptide thrombin inhibitor DuP 714 caused side effects in laboratory animals that appear to be related to its ability to inhi bit complement factor I, thereby activating the complement cascade. Us ing X-ray crystal structure information, we have designed compounds th at have greater selectivity for thrombin over factor I and that have r educed tendency to produce these side effects. (C) 1998 The DuPont Mer ck Pharmaceutical Company. Published by Elsevier Science Ltd.