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.
引用
收藏
页码：2795 / 2798
页数：4
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