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

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.

Keywords: PPARγ; bavachinin; diabetes mellitus; reporter gene assays; structure-activity relationships.