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

Peroxisome proliferator-activated receptor[gamma] (PPAR[gamma]) 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 PPAR[gamma] a...

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Published in:ChemMedChem 2017-01, Vol.12 (2), p.183
Main Authors: Du, Guoxin, Zhao, Yuanyuan, Feng, Li, Yang, Zhuo, Shi, Jiye, Huang, Cheng, Li, Bo, Guo, Fujiang, Zhu, Weiliang, Li, Yiming
Format: Article
Language:English
Subjects:
Glucose
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Summary:Peroxisome proliferator-activated receptor[gamma] (PPAR[gamma]) 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 PPAR[gamma] agonist activity. In this study, analogues of bavachinin were designed, synthesized, and evaluated by reporter gene assays for PPAR[gamma] agonist activity. Preliminary structure-activity relationships for these bavachinin analogues have been summarized, and seven compounds were found to have higher PPAR[gamma] agonist activities than the parent flavanone bavachinin.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201600554