[Synthesis and anti-inflammatory activity of hydroxylated E,E-1-(3'-indolyl)-5-(substituted phenyl)-1,4-pentadien-3-one derivatives].
2006
Aim A series of new 1,4-pentadien-3one derivatives were synthesized to search for new non-steroidal anti-inflammatory drugs(NSAIDs) with potent activity.Methods Eight 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 ~(1)H NMR,ESI-MS and element analysis.Their anti-inflammatory activity in vitro were evaluated.Results Preliminary in vitro pharmacological tests showed that all compounds exhibited anti-inflammatory activity.Conclusion Compounds 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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