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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 | |
| 引用本文： | 郭晓河,程森祥,程桂芳,谢晶曦,常俊标.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[J].药学学报,2006,41(4):346-351. |
| 作者姓名： | 郭晓河 程森祥 程桂芳 谢晶曦 常俊标 |
| 作者单位： | 1. 中国科学技术大学,化学系,安徽,合肥,230026 2. 河南省精细化工重点实验室,河南,郑州,450002 3. 中国医学科学院、中国协和医科大学药物研究所,北京,100050 4. 河南省精细化工重点实验室,河南,郑州,450002;河南省精细化工重点实验室,河南,郑州,450002 5. 中国科学技术大学,化学系,安徽,合肥,230026;河南省精细化工重点实验室,河南,郑州,450002 |
| 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。 |
| 关 键 词： | 合成 抗炎活性 羟基 吲哚 戊二烯酮化合物 |
| 文章编号： | 0513-4870（2006）04-0346-06 |
| 收稿时间： | 2005-08-04 |
| 修稿时间： | 2005-08-04 |
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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| 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 derivatives[J].Acta Pharmaceutica Sinica,2006,41(4):346-351. | |
| Authors: | GUO Xiao-he CHENG Sen-xiang CHENG Gui-fang XIE Jing-xi CHANG Jun-biao |
| Institution: | 1. Department of Chemistry , University of Science and Technology of China, Hefei 230026, China ; 2. Henan Key Laboratory of Fine Chemicals, Zhengzhou 450002, China; 2. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China |
| Abstract: | AIM: A series of new 1,4-pentadien-3-one derivatives were synthesized to search for new Eight novel hydroxylated non-steroidal anti-inflammatory drugs (NSAIDs) with potent activity. METHODS: 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. |
| Keywords: | synthesis anti-inflammatory activity hydroxylated indole pentadienone |
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