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新型(E)-1-取代苯基-3-(3’-取代吲哚基)-2-丙烯酮类化合物的合成和抗炎活性研究

郭晓河1,2, 程森祥3, 程桂芳4, 谢晶曦3, 常俊标1,2   

    1. 中国科学技术大学化学系, 合肥 230026;
    2. 新乡医学院, 新乡 453003;
    3. 河南省精细化工重点实验室, 郑州 450002;
    4. 中国医学科学院, 中国协和医科大学药物研究所, 北京 100051
  • 收稿日期:2005-09-05 修回日期:1900-01-01 出版日期:2006-09-10 发布日期:2006-09-10
  • 通讯作者: 常俊标

Synthesis and in vivo Antiinflammatory Activity of Novel E-1-substituted Phenyl-3-(3'-substituted indolyl)-2-propenones

GUO Xiao-He1,2, CHENG Sen-Xiang3, CHENG Gui-Fang4, XIE Jing-Xi3, CHANG Jun-Biao1,2   

    1. Department of Chemistry, University of Science and Technology of China, Hefei 230026, China;
    2. Xinxiang Medical University, Xinxiang 453003, China;
    3. Henan Key Laboratory of Fine Chemicals, Zhengzhou 450002, China;
    4. Institute of Materia Medica, Chinese Academy of Medical Sciences and Perking Union Medical College, Beijing 100051, China
  • Received:2005-09-05 Revised:1900-01-01 Online:2006-09-10 Published:2006-09-10
  • Contact: CHANG Jun-Biao

摘要: 设计合成了一系列新的丙烯酮化合物3a~3p, 其结构经1H NMR, IR, LC/MS确证. 用化合物对小鼠耳部巴豆油炎症影响的炎症模型测定化合物3a~3i的生物活性, 结果表明, 化合物3d, 3f, 3g可明显抑制巴豆油致小鼠耳部炎症. 其抑制率分别为19.5%, 27.6%, 16.1%.

关键词: 丙烯酮类化合物, 抗炎活性, 合成

Abstract: A series of novel propenylone compounds 3a—3p were designed and synthesized. The title compounds were characterized by 1H NMR, IR and LC/MS. Antiinflammatory activity of compounds 3a—3i were evaluated with a in vivo model of mice ear acute inflammation edema induced by croton oil. Compounds 3d, 3f, 3g exhibited a potent antiinflammatory activity and their inhibition ratios were 19.5%, 27.6% and 16.1%, respectively.

Key words: Synthesis, Anti-inflammatory activity, Propenone

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