Design, synthesis and bioactivity of novel phthalimide derivatives as acetylcholinesterase inhibitors
文献类型: 外文期刊
第一作者: Zhang, Tao
作者: Zhang, Tao;Zhang, Lanxiang;Mei, Xiangdong;Dong, Mengya;Zhang, Kaixin;Ning, Jun
作者机构:
关键词: Substructure combination;Phthalimide derivatives;Acetylcholinesterase inhibitor;Structure-activity relationship;Molecular docking
期刊名称:BIOORGANIC & MEDICINAL CHEMISTRY LETTERS ( 影响因子:2.823; 五年影响因子:2.677 )
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收录情况: SCI
摘要: A series of novel phthalimide derivatives related to benzylpiperazine were synthesized and evaluated as cholinesterase inhibitors. The results showed that all compounds were able to inhibit acetylcholinesterase (AChE), with two of them dramatically inhibiting butyrylcholinesterase (BuChE). Most compounds exhibited potent anti-AChE activity in the range of nM concentrations. In particular, compounds 7aIII and 10a showed the most potent activity with the IC50 values of 18.44 nM and 13.58 nM, respectively. To understand the excellent activity of these compounds, the structure-activity relationship was further examined. The protein-ligand docking study demonstrated that the target compounds have special binding modes and these results are in agreement with the kinetic study. (C) 2015 Elsevier Ltd. All rights reserved.
分类号: R9
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