Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.
A series of aromatic acetic acid compounds were designed and synthesized on the basis of Non-steroidal anti-inflammatory drugs indomethacin and diclofenac. Compounds 5a, 7a, 5h, 7h and 17 could strongly promote insulin-regulated differentiation of 3T3-L1 cells in vitro. They acted as full or partial PPARgamma agonist, or improved insulin resistance through non-PPARgamma pathway.
Zhang
Jiquan
J
School of Pharmacy, Guiyang Medical College, Guiyang 550004, China.
Wang
Jianta
J
Wu
Haoshu
H
He
Yaoyao
Y
Zhu
Gaofeng
G
Cui
Xing
X
Tang
Lei
L
D041721:3T3-L1 Cells; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology; D002454:Cell Differentiation / Q000187:drug effects; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D004008:Diclofenac / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D007213:Indomethacin / Q000737:chemistry / Q000494:pharmacology*; D007328:Insulin / Q000494:pharmacology; D007333:Insulin Resistance; D051379:Mice; D047495:PPAR gamma / Q000819:agonists / Q000378:metabolism; D051381:Rats
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D007328:Insulin; D047495:PPAR gamma; D004008:Diclofenac; D007213:Indomethacin