Abstract Peroxisome proliferator-activated receptor γ (PPARγ) is a transcriptional factor and key regulatory element in glucose and lipid metabolism. We have attempted to determine the structure–activity relationship between flavonoids as PPARγ agonists through a literature search. To compare results from different studies and methods, we have recalculated them to the percentage of positive control (% PC ). We have also described various methods used to determine PPARγ agonists. The most promising PPARγ agonists are isoflavones, namely 4'-fluoro-7-hydroxyisoflavone ( 4 ; % PC = 710.3%). The results presented in this review could be used for further semisynthetic modifications of flavonoids to enhance their PPARγ agonistic activity.