Synthesis and biological activity of a novel series of indole-derived PPARγ agonists

被引：35

作者：

Henke, BR

Adkison, KK

Blanchard, SG

Leesnitzer, LM

Mook, RA

Plunket, KD

Ray, JA

Roberson, C

Unwalla, R

Willson, TM

机构：

[1] Glaxo Wellcome Inc, Res & Dev, Dept Med Chem, Res Triangle Pk, NC 27709 USA

[2] Glaxo Wellcome Inc, Res & Dev, Dept Bioanal & Drug Metab, Res Triangle Pk, NC 27709 USA

[3] Glaxo Wellcome Inc, Res & Dev, Dept Mol Biochem, Res Triangle Pk, NC 27709 USA

[4] Glaxo Wellcome Inc, Res & Dev, Dept Mol Endocrinol, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(99)00603-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and structure-activity relationships of a novel series of indole 5-carboxylic acids that bind and activate peroxisome proliferator-activated receptor gamma (PPAR gamma) are reported. These new analogs are selective for PPAR gamma vs the other PPAR subtypes, and the most potent compounds in this series are comparable to in vitro potencies at PPAR gamma reported for the thiazolidinedione-based antidiabetic drugs currently in clinical use. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：3329 / 3334

页数：6

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