Design and synthesis of potent and subtype-selective PPARα agonists

被引：18

作者：

Desai, RC

Metzger, E

Santini, C

Meinke, PT

Heck, JV

Berger, JP

MacNaul, KL

Cai, TQ

Wright, SD

Agrawal, A

Moller, DE

Sahoo, SP

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Metab Disorders, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Cardiovasc Dis, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Drug Metab, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 06期

关键词：

PPAR alpha agonist;

D O I：

10.1016/j.bmcl.2005.12.022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Beginning with a moderately potent PPAR gamma agonist 9, a series of potent and highly subtype-selective PPAR alpha agonists was identified through a systematic SAR study. Based on the results of the efficacy studies in the hamster and dog models of dyslipidemia and the desired pharmacokinetic data, the optimized compound 39 was selected for further profiling. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：1673 / 1678

页数：6

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