5-aryl thiazolidine-2,4-diones:: Discovery of PPAR dual α/γ agonists as antidiabetic agents

被引：62

作者：

Desai, RC

Han, W

Metzger, EJ

Bergman, JP

Gratale, DF

MacNaul, KL

Berger, JP

Doebber, TW

Leung, K

Moller, DE

Heck, JV

Sahoo, SP

机构：

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

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(03)00505-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 5-aryl tliiazolidine-2,4-diones based dual PPARalpha/gamma agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：2795 / 2798

页数：4

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