(2R)-2-Methylchromane-2-carboxylic acids:: Discovery of selective PPARα agonists as hypolipidemic agents

被引：17

作者：

Koyama, H

Boueres, JK

Miller, DJ

Berger, JP

MacNaul, KL

Wang, PR

Ippolito, MC

Wright, SD

Agrawal, AK

Moller, DE

Sahoo, SP

机构：

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

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

[3] Merck Res Labs, Dept Atherosclerosis & Endocrinol, Rahway, NJ 07065 USA

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 14期

关键词：

PPAR; chromane-2-carboxylic acid; atherosclerosis;

D O I：

10.1016/j.bmcl.2005.05.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A SAR study was conducted on chromane-2-carboxylic acid toward selective PPAR alpha agonisim. As a result, highly potent, and selective PPAR alpha agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in hamster and dog animal models. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：3347 / 3351

页数：5

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