GUO Xiao-he, CHENG Sen-xiang, CHENG Gui-fang, XIE Jing-xi, CHANG Jun-biao. Synthesis and anti-inflammatory activity of hydroxylated E,E-1-(3′-indolyl)-5-(substituted phenyl)-1,4-pentadien-3-one derivativesJ. Acta Pharmaceutica Sinica, 2006, 41(4): 346-351.
Citation: GUO Xiao-he, CHENG Sen-xiang, CHENG Gui-fang, XIE Jing-xi, CHANG Jun-biao. Synthesis and anti-inflammatory activity of hydroxylated E,E-1-(3′-indolyl)-5-(substituted phenyl)-1,4-pentadien-3-one derivativesJ. Acta Pharmaceutica Sinica, 2006, 41(4): 346-351.

Synthesis and anti-inflammatory activity of hydroxylated E,E-1-(3′-indolyl)-5-(substituted phenyl)-1,4-pentadien-3-one derivatives

  • AimA series of new 1,4-pentadien-3-one derivatives were synthesized to search for new non-steroidal anti-inflammatory drugs (NSAIDs) with potent activity. MethodsEight novel hydroxylated E,E-1-(3′-indolyl)-5-(substituted phenyl)-1,4-pentadien-3-one derivatives were synthesized by means of aldol condensation and characterized by 1H NMR, ESI-MS and element analysis. Their anti-inflammatory activity in vitro were evaluated. ResultsPreliminary in vitro pharmacological tests showed that all compounds exhibited anti-inflammatory activity. ConclusionCompounds 4d and 4e exhibited potent anti-inflammatory activity and their anti-inflammatory activity was comparable to resveratrol, and were worthy of further study.
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