Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor γ (PPARγ) agonists

被引：28

作者：

Ahn, Jin Hee ^{[1
]}

Shin, Mi Sik

Jung, Sun Ho

Kim, Jin Ah

Kim, Hye Min

Kim, Se Hoan

Kanga, Seung Kyu

Kim, Kwang Rok

Dal Rhee, Sang

Park, Sung Dae

Lee, Jae Mok

Lee, Jeong Hyung

Cheon, Hyae Gyeong

Kim, Sung Soo

机构：

[1] Korea Res Inst Chem Technol, Bioorgan Sci Div, Taejon 305600, South Korea

[2] JEIL Pharmaceut Co Ltd, R&D Ctr, Yongin 449861, South Korea

[3] CJ Corp, R&D Ctr Pharmaceut, Ichon 467810, South Korea

[4] Korea Res Inst Chem Technol, Taejon 305333, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 18期

关键词：

PPAR gamma; indene N-oxide; diabetes; MURAGLITAZAR; MECHANISMS;

D O I：

10.1016/j.bmcl.2007.06.073

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel indene N-oxide derivatives were prepared by various synthetic methods and evaluated for their ability to activate PPAR gamma. The best PPAR gamma agonist in this series was 9 h, which showed an EC50 value of 15 nM. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5239 / 5244

页数：6

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