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新型乙酰胆碱酯酶抑制剂——豆腐果苷类似物的合成及生物学评价

Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.

作者信息

Wen Huan, Lin Chonglan, Que Ling, Ge Hui, Ma Lin, Cao Rihui, Wan Yiqian, Peng Wenlie, Wang Zihou, Song Huacan

机构信息

School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China.

出版信息

Eur J Med Chem. 2008 Jan;43(1):166-73. doi: 10.1016/j.ejmech.2007.03.018. Epub 2007 Apr 5.

DOI:10.1016/j.ejmech.2007.03.018
PMID:17574306
Abstract

A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent AChE inhibitory activities with IC(50) values of 0.45+/-0.02microM, 0.49+/-0.02microM, and 0.20+/-0.01microM, respectively. High selectivity for AChE over BuChE was also observed. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type.

摘要

制备了一系列的螺旋体类似物，并通过紫外光谱法在体外评估了它们对胆碱酯酶（乙酰胆碱酯酶和丁酰胆碱酯酶）的抑制活性。结果表明，化合物5、6d和8表现出较强的乙酰胆碱酯酶抑制活性，IC(50)值分别为0.45±0.02微摩尔、0.49±0.02微摩尔和0.20±0.01微摩尔。还观察到对乙酰胆碱酯酶的选择性高于丁酰胆碱酯酶。动力学研究表明，化合物5、6d和8对乙酰胆碱酯酶的抑制机制均为混合型。

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