Design, Synthesis, and Structure-Activity Relationships of Bavachinin Analogues as Peroxisome Proliferator-Activated Receptor γ Agonists

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• 作者：Dr. Guoxin Du ; Dr. Yuanyuan Zhao ; Dr. Li Feng ; Dr. Zhuo Yang ; Dr. Jiye Shi ; Prof. Cheng Huang ; Dr. Bo Li ; Dr. Fujiang Guo ; Prof. Weiliang Zhu and Prof. Yiming Li
• 刊名：ChemMedChem
• 出版年：2017
• 出版时间：January 20, 2017
• 年：2017
• 卷：12
• 期：2
• 页码：183-193
• 全文大小：691K
• ISSN：1860-7187

文摘

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.