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Novel ferulic amide derivatives with tertiary amine side chain as acetylcholinesterase and butyrylcholinesterase inhibitors: The influence of carbon spacer length, alkylamine and aromatic group

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成果类型:
期刊论文
作者:
Liu, Haoran;Liu, Linbo;Gao, Xiaohui;Liu, Yingzi*;Xu, Wanjun;...
通讯作者:
Liu, Yingzi
作者机构:
[Tang, Jingjing; Liu, Linbo; Liu, Haoran; Fan, Haoqun] Hunan Univ, Coll Chem & Chem Engn, Changsha 410082, Peoples R China.
[Xia, Xinhua; Gao, Xiaohui] Hunan Univ Chinese Med, Coll Pharm, Changsha 410208, Peoples R China.
[Xu, Wanjun; Liu, Yingzi; Jiang, Hong; He, Wei] Hunan Normal Univ, Coll Med, Changsha 410013, Peoples R China.
通讯机构:
[Liu, Yingzi] H
Hunan Normal Univ, Coll Med, Changsha 410013, Peoples R China.
语种:
英文
关键词:
Acetylcholinesterases;Alzheimer's disease;Ferulic acid;Molecular docking;alpha,beta-Unsaturated carbonyl
期刊:
European Journal of Medicinal Chemistry
ISSN:
0223-5234
年:
2017
卷:
126
页码:
810-822
基金类别:
innovative investigation funds for graduated students of Hu'nan province [HN2014082, CX2015B324]
机构署名:
本校为其他机构
院系归属:
药学院
摘要:
Based on our recent investigations on chalcone derivatives as AChE inhibitors, a series of ferulic acid (FA) tertiary amine derivatives similar to chalcone compounds were designed and synthesized. The results of bioactivity evaluation revealed that most of new synthesized compounds had comparable or more potent AChE inhibitory activity than the control drug Rivastigmine. The alteration of carbon chain linking tertiary amine groups and ferulic acid scaffold markedly influenced the inhibition activity against AChE. Among them the inhibitory activity of compound 6d (IC50: 0.71 +/- 0.09 mu mol/L) ...

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