The design and synthesis of a novel series of indole derived selective ETA antagonists

被引：36

作者：

Rawson, DJ ^{[1
]}

Dack, KN ^{[1
]}

Dickinson, RP ^{[1
]}

James, K ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)00660-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Conformational constraint has been used as the key design element in the identification of a series of potent and selective ETA antagonists. The most potent antagonist, 32, (ETA IC50 = 0.55 nM) is 722-fold selective over the ETB receptor, as measured by binding experiments. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：125 / 128

页数：4

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