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

Yao Xue Xue Bao

R&D Department, Chengdu Di'ao Pharmaceutical Group Co., LTD, Chengdu 610041, China.

Published: February 2005

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.

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