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


CONCLUSIONS
Compounds (1A and 3A) showed excellent insulin-sensitizing activities and should be worth further investigation.
Zhong
Chao-bin
CB
R&D Department, Chengdu Di'ao Pharmaceutical Group Co., LTD, Chengdu 610041, China.
Zhu
Xue-jun
XJ
Liu
Zhong-rong
ZR
Gao
Xiao-ping
XP
Wang
Xue-chao
XC
D041721:3T3-L1 Cells; D000818:Animals; D005947:Glucose / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000819:agonists / Q000138:chemical synthesis / Q000494:pharmacology; D007328:Insulin / Q000494:pharmacology; D007555:Isoxazoles / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D047495:PPAR gamma / Q000819:agonists / Q000138:chemical synthesis / Q000494:pharmacology
D007004:Hypoglycemic Agents; D007328:Insulin; D007555:Isoxazoles; D047495:PPAR gamma; D005947:Glucose; C112329:JTT 501