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用于治疗阿尔茨海默病的选择性丁酰胆碱酯酶抑制剂鉴定方面的最新进展。

Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease.

作者信息

Li Qi, Yang Hongyu, Chen Yao, Sun Haopeng

机构信息

Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.

出版信息

Eur J Med Chem. 2017 May 26;132:294-309. doi: 10.1016/j.ejmech.2017.03.062. Epub 2017 Mar 27.

Abstract

Alzheimer's disease (AD) is one of the most prevalent neurodegenerative disorders with notable factor of dysfunction in cholinergic system. Low ACh level can be observed in the pathogenesis of AD. Several AChE inhibitors have already been used for clinical treatments. However, other than normal conditions, ACh is mostly hydrolyzed by BuChE in progressed AD. Account for an increased level of BuChE and decreased level of AChE in the late stage of AD, development of selective BuChE inhibitor is of vital importance. Up till now, compounds with various scaffolds have been discovered to selectively inhibit BuChE. Different effective anti-BuChE molecules are concluded in this review.

摘要

阿尔茨海默病(AD)是最常见的神经退行性疾病之一,胆碱能系统功能障碍是其显著因素。在AD的发病机制中可观察到乙酰胆碱(ACh)水平降低。几种乙酰胆碱酯酶(AChE)抑制剂已用于临床治疗。然而,在进展性AD中,除正常情况外,ACh大多由丁酰胆碱酯酶(BuChE)水解。鉴于AD晚期BuChE水平升高而AChE水平降低,开发选择性BuChE抑制剂至关重要。到目前为止,已发现具有各种骨架的化合物可选择性抑制BuChE。本文综述了不同的有效抗BuChE分子。

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