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2-苯氧基茚满-1-酮衍生物作为乙酰胆碱酯酶抑制剂的设计、合成与评价

Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.

作者信息

Sheng Rong, Lin Xiao, Li Jingya, Jiang Yanke, Shang Zhicai, Hu Yongzhou

机构信息

ZJU-ENS Joint Laboratory of Medicinal Chemistry, Zhejiang University, Hubin Campus, Hangzhou 310031,China.

出版信息

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3834-7. doi: 10.1016/j.bmcl.2005.05.132.

Abstract

A series of 2-phenoxy-indan-1-one derivatives have been designed, synthesized, and tested as acetylcholinesterase inhibitors. The most potent compound exhibited high AChE inhibitory activity (IC50 = 50 nM), and the molecular docking study indicated that it was nicely accommodated by AChE.

摘要

设计、合成并测试了一系列2-苯氧基茚满-1-酮衍生物作为乙酰胆碱酯酶抑制剂。最有效的化合物表现出高乙酰胆碱酯酶抑制活性(IC50 = 50 nM),分子对接研究表明它能很好地被乙酰胆碱酯酶容纳。

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