Potent, selective benzenesulfonamide agonists of the human β3 adrenergic receptor

被引：32

作者：

Weber, AE ^{[1
]}

Mathvink, RJ

Perkins, L

Hutchins, JE

Candelore, MR

Tota, L

Strader, CD

Wyvratt, MJ

Fisher, MH

机构：

[1] Merck Res Labs, Dept Med Chem & Biochem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Mol Pharmacol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(98)00169-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A cloned human beta(3) adrenergic receptor assay was used to identify phenoxypropanolamine agonist 1. SAR studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM beta(3) agonist which shows 30-fold selectivity for beta(3) agonist activity over beta(1) and beta(2) receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over beta(1) and beta(2), respectively. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1101 / 1106

页数：6

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