Human β3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides

被引：217

作者：

Brockunier, LL ^{[1
]}

Parmee, ER

Ok, HO

Candelore, MR

Cascieri, MA

Colwell, LF

Deng, LP

Feeney, WP

Forrest, MJ

Hom, GJ

MacIntyre, DE

Tota, L

Wyvratt, MJ

Fisher, MH

Weber, AE

机构：

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

[2] Merck Res Labs, Dept Biochem & Physiol, Rahway, NJ 07065 USA

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

[4] Merck Res Labs, Dept Comparat Med, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)00422-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Compounds containing a 1,2,3-triazole-substituted benzenesulfonamide were prepared and found to be potent and selective human beta(3)-adrenergic receptor agonists. The most interesting compound, trifluoromethylbenzyl analogue 12e (beta(3) EC50 = 3.1 nM with >1500-fold selectivity over binding to both beta(1)- and beta(2) receptors), stimulates lipolysis in the rhesus monkey (ED50 = 0.36 mg/kg) and is 25% orally bioavailable in the dog. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2111 / 2114

页数：4

共 18 条

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