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论文 |
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论文题目: |
Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of human acetylcholinesterase and butyrylcholinesterase
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论文题目英文: |
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作者: |
Wang, Yue-Hu; Wan, Qin-Li; Gu, Cheng-Ding; Luo, Huai-Rong; Long, Chun-Lin
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论文出处: |
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2012
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卷: |
6 |
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发表期刊: |
CHEMISTRY CENTRAL JOURNAL |
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摘要: |
Background: Alzheimer's disease (AD) is a neurologically degenerative disorder that affects more than 20 million people worldwide. The selective butyrylcholinesterase (BChE) inhibitors and bivalent cholinesterase (ChE) inhibitors represent new treatments for AD. Findings: A series of lycorine derivatives (1-10) were synthesized and evaluated for anti-cholinesterase activity. Result showed that the novel compound 2-O-tert-butyldimethylsilyl-1-O-(methylthio) methyllycorine (7) was a dual inhibitor of human acetylcholinesterase (hAChE) and butyrylcholinesterase (hBChE) with IC50 values of 11.40 +/- 0.66 mu M and 4.17 +/- 0.29 mu M, respectively. The structure-activity relationships indicated that (i) the 1-O-(methylthio) methyl substituent in lycorine was better than the 1-O-acetyl group for the inhibition of cholinesterase; (ii) the acylated or etherified derivatives of lycorine and lycorin-2-one were more potent against hBChE than hAChE; and (iii) the oxidation of lycorine at C-2 decreases the activity. Conclusion: Acylated or etherified derivatives of lycorine are potential dual inhibitors of hBChE and hAChE. Hence, further study on the modification of lycorine for ChE inhibition is necessary. |
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