Identification of a series of PPAR-γ/δ dual agonists via solid-phase parallel synthesis

被引：41

作者：

Liu, KG

Lambert, MH

Leesnitzer, LM

Oliver, W

Ott, RJ

Plunket, KD

Stuart, LW

Brown, PJ

Willson, TM

Sternbach, DD ^{[1
]}

机构：

[1] GlaxoSmithKline, Nucl Receptor Discovery Res, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline, Metab Dis Drug Discovery, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(01)00596-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have developed a general solid-phase synthesis for identification of PPAR ligands. Synthesis of a 480-member library led to the identification of a potent PPAR gamma/delta dual agonist 23. Compound 23 showed good plasma exposure in rats and demonstrated antihyperglycemic and antihyperlipidemic efficacy in diabetic fatty Zucker rats. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2959 / 2962

页数：4

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