Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: Structures based on the (D)-Arg-Gly-Arg tripeptide sequence

Authors
Marlowe, CK Sinha, U Gunn, AC Scarborough, RM
Citation
Ck. Marlowe et al., Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: Structures based on the (D)-Arg-Gly-Arg tripeptide sequence, BIOORG MED, 10(1), 2000, pp. 13-16
Citations number
19
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
1
Year of publication
2000
Pages
13 - 16
Database
ISI
SICI code
0960-894X(20000103)10:1<13:DSASRO>2.0.ZU;2-W
Abstract
A series of arginine aldehyde inhibitors was designed as transition state ( TS) analogues based on the known factor Xa specific substrate Cbz-D-Arg-Gly -Arg-pNA. BnSO2-(D)Arg-Gly-Arg-H (20) was found to be the most potent and s elective inhibitor of factor Xa and prothrombinase activity in this series. (C) 1999 Elsevier Science Ltd. All rights reserved.