Potent, selective human β3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore

被引：58

作者：

Mathvink, RJ ^{[1
]}

Barritta, AM

Candelore, MR

Cascieri, MA

Deng, LP

Tota, L

Strader, CD

Wyvratt, MJ

Fisher, MH

Weber, AE

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 | 1999年 / 9卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(99)00277-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of compounds possessing an N-substituted indoline-5-sulfonamide pharmacophore was prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. The SAR of a wide range of urea and heterocyclic substituents is discussed. 4-Octyl thiazole compound 8c was the most potent and selective compound in the series, with 2800-fold selectivity over beta(1) binding and 1400-fold selectivity over beta(2) binding (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1869 / 1874

页数：6

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