Design and synthesis of 2-methyl-2-{4-[2-(5-methyl-2-aryloxazol-4-yl)ethoxy]phenoxy}propionic acids:: A new class of dual PPARα/γ agonists

被引：76

作者：

Brooks, DA ^{[1
]}

Etgen, GJ

Rito, CJ

Shuker, AJ

Dominianni, SJ

Warshawsky, AM

Ardecky, R

Paterniti, JR

Tyhonas, J

Karanewsky, DS

Kauffman, RF

Broderick, CL

Oldham, BA

Montrose-Rafizadeh, C

Winneroski, LL

Faul, MM

McCarthy, JR

机构：

[1] Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

[2] Ligand Pharmaceut Inc, San Diego, CA 92121 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 13期

关键词：

D O I：

10.1021/jm0155188

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Propionic acid derivative 8, which was designed and synthesized based on putative pharmacophores of known PPAR gamma- and PPAR alpha -selective compounds, exhibits potent dual PPAR alpha/gamma agonist activity as demonstrated by in vitro binding and dose overlap in the newly introduced EOB mouse model for glucose lowering and lipid/cholesterol homeostasis.

引用

页码：2061 / 2064

页数：4

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