[Design, synthesis and insulin-sensitizing activity of some peroxisome proliferator-activated gamma agonists].

AIM: To find new peroxisome proliferator-activated y agonists with high activity and low toxicity. METHODS: Based on JTT-501 and JTT-20993, new isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds were designed and synthesized. Their insulin-sensitizing activities were evaluated. RESULTS: Eight new compounds were obtained. The structures of synthesized compounds were characterized by NMR, MS and IR. Four compounds (1A-4A) showed insulin-sensitizing activities. CONCLUSION: Compounds (1A and 3A) showed excellent insulin-sensitizing activities and should be worth further investigation.