过氧化物酶体增殖物激活受体
化学
受体
过氧化物酶体
过氧化物酶体增殖物
药理学
过氧化物酶体增殖物激活受体α
过氧化物酶体增殖物激活受体γ
结构-活动关系
生物化学
立体化学
核受体
生物
转录因子
体外
基因
作者
Guoxin Du,Yuanyuan Zhao,Feng Li,Zhuo Yang,Jiye Shi,Cheng Huang,Bo Li,Fujiang Guo,Weiliang Zhu,Yiming Li
出处
期刊:ChemMedChem
[Wiley]
日期:2016-12-03
卷期号:12 (2): 183-193
被引量:20
标识
DOI:10.1002/cmdc.201600554
摘要
Abstract Peroxisome proliferator‐activated receptor γ (PPARγ) agonists have been used for the treatment of diabetes with the effect of lowering blood glucose levels and improving insulin sensitivity. Natural compounds such as flavones, flavanones, and isoflavones have shown excellent PPARγ agonist activity. In this study, analogues of bavachinin were designed, synthesized, and evaluated by reporter gene assays for PPARγ agonist activity. Preliminary structure–activity relationships for these bavachinin analogues have been summarized, and seven compounds were found to have higher PPARγ agonist activities than the parent flavanone bavachinin.
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