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有机化学
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有机化学 ›› 2013, Vol. 33 ›› Issue (03): 621-629.DOI: 10.6023/cjoc201210042 上一篇    下一篇

研究论文

染料木素氨基甲酸酯类衍生物的合成及生物活性研究

强晓明a, 袁文a, 桑志培a, 邓勇a,b   

  1. a 四川大学华西药学院药物化学系 成都 610041;
    b 四川大学华西药学院 靶向药物及释药系统教育部重点实验室 成都 610041
  • 收稿日期:2012-10-22 修回日期:2012-11-10 发布日期:2012-11-23
  • 通讯作者: 邓勇 E-mail:dengyongy@sohu.com
  • 基金资助:

    国家自然科学基金(Nos. 20672077, 20872099)、教育部博士点基金(No. 20110181110079)和国家科技重大专项(No. 2013ZX09301304-002)资助项目.

Synthesis and Biological Evaluation of Genistein Carbamate Derivatives

Qiang Xiaominga, Yuan Wena, Sang Zhipeia, Deng Yonga,b   

  1. a Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041;
    b Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041
  • Received:2012-10-22 Revised:2012-11-10 Published:2012-11-23
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 20672077, 20872099), the Research Fund for the Doctoral Program of Higher Education (No. 20110181110079) and the National Science and Technology Major Project (No. 2013ZX09102-012).

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基于多靶点药物设计策略, 以染料木素为先导化合物, 对其7-位和4'-位羟基进行修饰, 合成了24个染料木素氨基甲酸酯类衍生物, 其化学结构经1H NMR和HRMS确证. 生物活性测试结果表明, 部分化合物对乙酰胆碱酯酶具有较强抑制活性, 且对H2O2诱导的PC12细胞氧化损伤具有显著保护作用.

With genistein as lead compound, twenty-four genistein carbamate derivatives were synthesized from genistein with the structural modification of 7-OH and 4'-OH based on the muti-target-directed drug design strategy. The chemical structures of target compounds were confirmed by 1H NMR and HRMS techniques. Their acetylcholinesterase and butylcholinesterase inhibitory activity and neuroprotective effects against hydrogen peroxide induced PC12 cell injury were evaluated in vitro. The results indicated that some compounds exhibited the most potent acetylcholinesterase inhibitory activity and neuroprotective effects.

Key words: alzheimer’s disease, muti-target therapeutics, genistein carbamate derivatives, synthesis, AChE inhibitors, neuroprotective agents