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Chinese Journal of Organic Chemistry >

2013 , Vol. 33 >Issue 03: 621 - 629

DOI: https://doi.org/10.6023/cjoc201210042

Articles

Synthesis and Biological Evaluation of Genistein Carbamate Derivatives

  • Qiang Xiaoming ,
  • Yuan Wen ,
  • Sang Zhipei ,
  • Deng Yong
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  • 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 date: 2012-10-22

  Revised date: 2012-11-10

  Online 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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Abstract

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

Cite this article

Qiang Xiaoming , Yuan Wen , Sang Zhipei , Deng Yong . Synthesis and Biological Evaluation of Genistein Carbamate Derivatives[J]. Chinese Journal of Organic Chemistry, 2013 , 33(03) : 621 -629 . DOI: 10.6023/cjoc201210042

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