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茚满二酮和噢哢衍生物的设计、合成及乙酰胆碱酯酶抑制活性

Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.

作者信息

Sheng Rong, Xu Yu, Hu Chunqi, Zhang Jing, Lin Xiao, Li Jingya, Yang Bo, He Qiaojun, Hu Yongzhou

机构信息

ZJU-ENS joint laboratory of Medicinal Chemistry, School of Pharmaceutical Sciences, Zijingang Campus, Zhejiang University Hangzhou 310058, People's Republic of China.

出版信息

Eur J Med Chem. 2009 Jan;44(1):7-17. doi: 10.1016/j.ejmech.2008.03.003. Epub 2008 Mar 16.

DOI:10.1016/j.ejmech.2008.03.003
PMID:18436348
Abstract

A new series of indanone and aurone derivatives have been synthesized and tested for in vitro AChE inhibitory activity by modified Ellman method. Most of them exhibit AChE inhibitory activities superior to rivastigmine. Further, the most potent compound 1g was selected to evaluate the effect on the acquisition and memory impairment by mice step-down passive avoidance test.

摘要

已合成了一系列新的茚满二酮和橙酮衍生物，并通过改良的Ellman方法测试了它们的体外乙酰胆碱酯酶抑制活性。其中大多数表现出优于 rivastigmine 的乙酰胆碱酯酶抑制活性。此外，选择了最有效的化合物 1g，通过小鼠被动回避试验评估其对习得和记忆损伤的影响。

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