The de novo design and synthesis of cyclic urea inhibitors of factor Xa: Optimization of the S4 ligand

Authors
Galemmo, RA Wells, BL Rossi, KA Alexander, RS Dominguez, C Maduskuie, TP Stouten, PFW Wright, MR Aungst, BJ Wong, PC Knabb, RM Wexler, RR
Citation
Ra. Galemmo et al., The de novo design and synthesis of cyclic urea inhibitors of factor Xa: Optimization of the S4 ligand, BIOORG MED, 10(3), 2000, pp. 301-304
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
3
Year of publication
2000
Pages
301 - 304
Database
ISI
SICI code
0960-894X(20000207)10:3<301:TDNDAS>2.0.ZU;2-O
Abstract
In this report refinements to the S4 ligand group leads to compound 19, an inhibitor of fXa with good potency in vitro and an improved pharmacokinetic profile in rabbit. The X-ray crystallographic study of a representative an alogue confirms our binding model for this series. (C) 2000 DuPont Pharmace uticals Company. Published by Elsevier Science Ltd. All rights reserved.