1,3,5-Trisubstituted aryls as highly selective PPARδ agonists

被引：37

作者：

Epple, R

Azimioara, M

Russo, R

Bursulaya, B

Tian, SS

Gerken, A

Iskandar, M

机构：

[1] Novartis Res Fdn, Genom Inst, Dept Med Chem, San Diego, CA 92121 USA

[2] Novartis Res Fdn, Genom Inst, Dept Biol Struct, San Diego, CA 92121 USA

[3] Novartis Res Fdn, Genom Inst, Dept Lead Discovery, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 11期

关键词：

nuclear receptors; peroxisome proliferator-activated receptor delta; PPAR agonists; virtual docking;

D O I：

10.1016/j.bmcl.2006.02.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of highly potent and selective PPAR delta agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes lip to 10 mu M, making it a useful tool in studying the biological effects of selective PPAR delta activation. (c) 2006 Elsevier Ltd. All rights reserved.

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收藏

页码：2969 / 2973

页数：5

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