化学
药效团
恶唑
羧酸
部分
兴奋剂
体内
过氧化物酶体增殖物激活受体
激活剂(遗传学)
立体化学
体外
铅化合物
组合化学
对接(动物)
生物利用度
受体
生物化学
药理学
医学
生物技术
生物
护理部
作者
Harikishore Pingali,Mukul R. Jain,Shailesh R. Shah,Pankaj Makadia,Pandurang Zaware,Jeevankumar Jamili,K Sairam,Pravin Patil,Dinesh Suthar,Suresh Giri,H. H. Patel,Pankaj R. Patel
出处
期刊:Letters in Drug Design & Discovery
[Bentham Science]
日期:2010-05-16
卷期号:7 (6): 421-429
被引量:1
标识
DOI:10.2174/157018010791306533
摘要
1,3-dioxane carboxylic acid derivatives were prepared based on our previous studies directed towards identifying novel pharmacophore for the development of PPAR α/γ dual agonists. Based on the typical topology of PPAR agonists we focused our design approach on modifying lipophilic tail and prepared a series of compounds by replacing the oxazole moiety of our previously reported compound with optimized lipophilic groups. Compound 8a was found to be a weak PPAR activator but exhibited potent hypolipidemic and anti-hyperglycemic activities in vivo due to superior bioavailability, whereas 8f exhibited potent in vitro and invivo effects. The activity of 8f is further supported by molecular docking study. Keywords: PPAR agonist, PPAR α/γ dual agonists, Type 2 diabetes, 1,3-dioxane carboxylic acid
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