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Design, Synthesis, and Structure–Activity Relationships of Bavachinin Analogues as Peroxisome Proliferator‐Activated Receptor γ Agonists
Author(s) -
Du Guoxin,
Zhao Yuanyuan,
Feng Li,
Yang Zhuo,
Shi Jiye,
Huang Cheng,
Li Bo,
Guo Fujiang,
Zhu Weiliang,
Li Yiming
Publication year - 2017
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201600554
Subject(s) - agonist , flavones , peroxisome proliferator activated receptor , chemistry , isoflavones , flavanone , receptor , peroxisome , partial agonist , pharmacology , biochemistry , medicine , endocrinology , biology , flavonoid , antioxidant , chromatography
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.