Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human β3 adrenergic receptor agonists

被引：17
作者：
Parmee, ER [1 ]
Brockunier, LL
He, JF
Singh, SB
Candelore, MR
Cascieri, MA
Deng, LP
Liu, Y
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 Mol Syst, Rahway, NJ 07065 USA
[3] Merck Res Labs, Dept Biochem & Mol Pharmacol, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(00)00459-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta (3) adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta (3) AR. Naphthyloxy compound 18 (beta (3) EC50 = 78 nM) did not activate the beta (1) and beta (2) ARs at 10 muM, and showed >1000-fold selectivity over binding to the beta (1) and beta (2) ARs. (C) 2000 Elsevier Science Ltd. All rights reserved.
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页码：2283 / 2286
页数：4
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