To explore novel peroxisome proliferator-activated receptor (PPAR) agonists with high efficacy and low toxicity, thirteen new β-amino ketone derivatives containing a sulfamethoxazole moiety were synthesized directly through Mannich reaction in the yields of 39.8%～92.5%. Their structures were characterized by IR, 1H NMR, 13C NMR, ESI MS and HRMS techniques. The preliminary bioassay showed that compound 1a could activate PPAR response element obviously. The reaction conditions and the structure-activity relationship of these compounds were also discussed.

Key words: PPAR, Mannich reaction, β-amino ketone derivative, diabetes mellitus, sulfamethoxazole