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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

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

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【Author】 GUO Xiao-he~(1),CHENG Sen-xiang~(2),CHENG Gui-fang~(3),XIE Jing-xi~(2,3),CHANG Jun-biao~(1,2*)(1.Department of Chemistry,University of Science and Technology of China,Hefei 230026,China;2.Henan Key Laboratory of Fine Chemicals,Zhengzhou 450002,China;3.Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)

【机构】中国科学技术大学化学系；河南省精细化工重点实验室；中国医学科学院中国协和医科大学药物研究所；中国科学技术大学化学系安徽合肥230026；河南郑州450002；北京100050；中国医学科学院；中国协和医科大学药物研究所；安徽合肥230026；

【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4 e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。更多还原

【Abstract】 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 ¹H 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.更多还原

【关键词】合成；抗炎活性；羟基；吲哚；戊二烯酮化合物；
【Key words】 synthesis； anti-inflammatory activity； hydroxylated； indole； pentadienone；

【基金】国家自然科学基金资助项目(29972009).

【文献出处】药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,2006年04期

【分类号】R914
【被引频次】28
【下载频次】328

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