石杉碱乙衍生物的合成及其对乙酰胆碱酯酶的抑制作用
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
作者信息
Feng Song, Xia Yu, Han Dongmei, Zheng Chunyan, He Xuchang, Tang Xican, Bai Donglu
机构信息
State Key Laboratory for New Drug Research, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.
出版信息
Bioorg Med Chem Lett. 2005 Feb 1;15(3):523-6. doi: 10.1016/j.bmcl.2004.11.060.
PMID:15664805
Abstract
By targeting dual active sites of AChE, a number of new derivatives of HupB have been synthesized and tested as acetylcholinesterase inhibitors. The most potent compound, bis-HupB 5b is 72-fold more potent in AChE inhibition and 79-fold more selective for AChE versus BChE than HupB.
摘要
通过靶向乙酰胆碱酯酶（AChE）的两个活性位点，已经合成了许多石杉碱甲（HupB）的新衍生物，并作为乙酰胆碱酯酶抑制剂进行了测试。最有效的化合物双石杉碱甲5b在抑制AChE方面比石杉碱甲强72倍，对AChE相对于丁酰胆碱酯酶（BChE）的选择性比石杉碱甲高79倍。
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