Thromboxane modulating agents. 4. Design and synthesis of 3-(2-[{(4-chlorophenyl)sulfonyl}-amino]ethyl)benzenepropanoic acid derivatives as potent thromboxane receptor antagonists.

被引：9

作者：

Dack, KN ^{[1
]}

Dickinson, RP

Long, CJ

Steele, J

机构：

[1] Pfizer Ltd, Cent Res, Dept Discovery Chem, Sandwich CT13 9NJ, Kent, England

[2] Pfizer Ltd, Cent Res, Dept Discovery Biol, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(98)00242-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design of a series of thromboxane receptor antagonists based on 3-(2-[{(4-chlorophenyl)sulfonyl}amino]ethyl)benzenepropanoic acid (1) is described. Addition of an arylmethyl group at the 5-position of 1 gave exceptionally potent agents in vitro and in vivo, with 13a (UK-147,535) giving complete blockade of the TxA(2) receptor for greater than 12 hours in dogs, following all oral dose of 0.1 mg/kg. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2061 / 2066

页数：6