新型含羟基<i>E,E</i>-1-(3′-吲哚基)-5-取代苯基-1，4-戊二烯-3-酮化合物的合成及抗炎活性

新型含羟基E,E-1-(3′-吲哚基)-5-取代苯基-1，4-戊二烯-3-酮化合物的合成及抗炎活性

摘要: 目的寻找新的非甾体抗炎药物。方法利用羟醛缩合反应，合成了8个新型含羟基的E,E-1-(3′-吲哚基)-5-取代苯基-1，4-戊二烯-3-酮化合物，通过¹H NMR，ESI-MS和元素分析对其结构进行表征。并测定了体外抗炎活性。结果体外抗炎活性测试结果表明，所有化合物都有一定程度的抗炎活性。结论其中化合物4d和4e具有较强的抗炎活性，其抗炎活性与白藜芦醇接近，值得进一步研究。

Abstract: 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.