Synthesis and biological activities of novel indole derivatives as potent and selective PPARγ modulators

被引：48

作者：

Lamotte, Yann ^{[1
]}

Martres, Paul ^{[1
]}

Faucher, Nicolas ^{[1
]}

Laroze, Alain ^{[1
]}

Grillot, Didier ^{[2
]}

Ancellin, Nicolas ^{[2
]}

Saintillan, Yannick ^{[2
]}

Beneton, Veronique ^{[3
]}

Gampe, Robert T., Jr. ^{[4
]}

机构：

[1] Lab GlaxoSmithKline, Ctr Rech, Dept Med Chem, F-91951 Les Ulis, France

[2] Lab GlaxoSmithKline, Ctr Rech, Dept Biol, F-91951 Les Ulis, France

[3] Lab GlaxoSmithKline, Dept Drugs Metab & Pharmacokinet, Ctr Rech, F-91951 Les Ulis, France

[4] GlaxoSmithKline, Dept Computat & Struct Chem, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 04期

关键词：

PPAR gamma; Peroxisome proliferator-activated receptor; Telmisartan; Diabetes; Modulator; ACTIVATED RECEPTOR-GAMMA; AGONISTS; DISCOVERY; SERIES; ANTAGONISTS; BINDING; DELTA;

D O I：

10.1016/j.bmcl.2009.12.107

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from the structure of Telmisartan, a new series of potent and selective PPAR gamma modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds are reported and the X-ray structure of compound 7b bound to the PPAR gamma ligand binding domain is described. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1399 / 1404

页数：6

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