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

被引：13

作者：

Galemmo, RA ^{[1
]}

Wells, BL ^{[1
]}

Rossi, KA ^{[1
]}

Alexander, RS ^{[1
]}

Dominguez, C ^{[1
]}

Maduskuie, TP ^{[1
]}

Stouten, PFW ^{[1
]}

Wright, MR ^{[1
]}

Aungst, BJ ^{[1
]}

Wong, PC ^{[1
]}

Knabb, RM ^{[1
]}

Wexler, RR ^{[1
]}

机构：

[1] Dupont Pharmaceut Co, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(99)00688-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 analogue confirms our binding model for this series. (C) 2000 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：301 / 304

页数：4

共 23 条

[1]

Bona RD, 1997, THROMB HAEMOSTASIS, V78, P137

[2] AROMATIC-AROMATIC INTERACTION - A MECHANISM OF PROTEIN-STRUCTURE STABILIZATION [J].