Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.

Abstract

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.

• Authors: Jiquan Zhang, Jianta Wang, Haoshu Wu, Yaoyao He, Gaofeng Zhu, Xing Cui, Lei Tang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 12 Pg. 3324-7 (Jun 15 2009) ISSN: 1464-3405 [Electronic] England
• PMID: 19423341 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anti-Inflammatory Agents, Non-Steroidal
• Cyclooxygenase Inhibitors
• Insulin
• PPAR gamma
• Diclofenac
• Indomethacin

Topics

• 3T3-L1 Cells
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (chemistry, pharmacology)
• Cell Differentiation (drug effects)
• Cyclooxygenase Inhibitors (chemistry, pharmacology)
• Diclofenac (chemistry, pharmacology)
• Drug Design
• Indomethacin (chemistry, pharmacology)
• Insulin (pharmacology)
• Insulin Resistance
• Mice
• PPAR gamma (agonists, metabolism)
• Rats