A series of novel 2, 4, 6-trisubstitutedpyrimidine-5-carboxylic acid derivatives were designed and synthesized with the intent of producing a peroxisome proliferator-activated receptor γ (PPARγ) partial agonist for antidiabetic agents. A pharmacophore-driven approach of in- house screening identified compound 7, which led to the identification of compound 9 featuring a 2, 4, 6-trisubstituted pyrimidine-5-carboxylic acid core. Structure− activity ...