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

AbstractA 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.
AuthorsJiquan Zhang, Jianta Wang, Haoshu Wu, Yaoyao He, Gaofeng Zhu, Xing Cui, Lei Tang (Affiliation: School of Pharmacy, Guiyang Medical College, Guiyang 550004, China.)
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 12 Pg. 3324-7 (Jun 15 2009) ISSN: 1464-3405 [Electronic] England
PMID19423341 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase Inhibitors
  • PPAR gamma
  • Insulin
  • 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