Journal
CHINESE JOURNAL OF ORGANIC CHEMISTRY
Volume 33, Issue 3, Pages 621-629Publisher
SCIENCE PRESS
DOI: 10.6023/cjoc201210042
Keywords
alzheimer's disease; mud-target therapeutics; genistein carbamate derivatives; synthesis; AChE inhibitors; neuroprotective agents
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Funding
- National Natural Science Foundation of China [20672077, 20872099]
- Research Fund for the Doctoral Program of Higher Education [20110181110079]
- National Science and Technology Major Project [2013ZX09102-012]
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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 H-1 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.
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