Synthesis and evaluation of potent and selective β3 adrenergic receptor agonists containing heterobiaryl carboxylic acids

被引：20
作者：
Shearer, Barry G. [1 ]
Chao, Esther Y.
Uehling, David E.
Deaton, David N.
Cowan, Conrad
Sherman, Bryan W.
Milliken, Tula
Faison, Walter
Brown, Kathleen
Adkison, Kimberly K.
Lee, Frank
机构：
[1] GlaxoSmithKline Inc, Dept Med Chem, Res Triangle Pk, NC 27709 USA
[2] GlaxoSmithKline Inc, Dept Receptor Biol, Res Triangle Pk, NC 27709 USA
[3] GlaxoSmithKline Inc, Dept Pharmacol, Res Triangle Pk, NC 27709 USA
[4] GlaxoSmithKline Inc, Dept Res Bioanal & Drug Metab, Res Triangle Pk, NC 27709 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 16期
关键词：
beta(3) adrenergic receptor; agonist; selective; diabetes;
D O I：
10.1016/j.bmcl.2007.05.069
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The design, synthesis, and SAR of a novel series of heterobiaryl phenethanolamine beta(3) adrenergic receptor agonists are described. The furan analogue 49 was shown to elicit a significant dose-dependent lowering of plasma glucose in a rodent model of type 2 diabetes. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4670 / 4677
页数：8
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