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.

引用

页码：2283 / 2286

页数：4

共 24 条

[1]

Arch JRS, 1996, INT J OBESITY, V20, P191

[2]

BROCKUNIER LL, 2000, Patent No. 6043253

[3] Synthesis and evaluation of trimetoquinol derivatives: Novel thromboxane A(2) prostaglandin H-2 antagonists with diminished beta-adrenergic agonist activity [J].