The de novo design and synthesis of cyclic urea inhibitors of Factor Xa: Initial SAR studies

被引：22

作者：

Galemmo, RA ^{[1
]}

Maduskuie, TP ^{[1
]}

Dominguez, C ^{[1
]}

Rossi, KA ^{[1
]}

Knabb, RM ^{[1
]}

Wexler, RR ^{[1
]}

Stouten, PFW ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00471-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this report we discuss the design, synthesis, rind validation of a novel series of cyclic urea inhibitors of the blood coagulation protein Factor Xa. This work culminates in compound 11, a mono-amidine inhibitor of fXa employing a new S4 ligand that reduces the cationic character of these analogs. Compound 11 represents a lead for a series of more potent and selective inhibitors. (C) 1998 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：2705 / 2710

页数：6

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