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Tertiary amine derivatives of chlorochalcone as acetylcholinesterase (AChE) and buthylcholinesterase (BuChE) inhibitors: the influence of chlorine, alkyl amine side chain and alpha,beta-unsaturated ketone group

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成果类型:
期刊论文
作者:
Gao, Xiao-hui;Zhou, Chao;Liu, Hao-ran*;Liu, Lin-bo;Tang, Jing-jing;...
通讯作者:
Xia, Xin-hua;Liu, Hao-ran
作者机构:
[Xia, Xin-hua; Gao, Xiao-hui] Hunan Univ Chinese Med, Coll Pharm, Changsha, Hunan, Peoples R China.
[Liu, Hao-ran; Liu, Lin-bo; Tang, Jing-jing; Zhou, Chao] Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.
通讯机构:
[Xia, Xin-hua; Liu, Hao-ran] H
Hunan Univ Chinese Med, Coll Pharm, Changsha, Hunan, Peoples R China.
Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.
语种:
英文
关键词:
*Acetylcholinesterase inhibitors;*Alzheimer's disease;*chlorochalcones;*pyrazoline;*structure-activity relationship
期刊:
Journal of Enzyme Inhibition and Medicinal Chemistry
ISSN:
1475-6366
年:
2017
卷:
32
期:
1
页码:
146-152
基金类别:
innovative investigation funds for post-graduated students of Hunan province [CX2015424]
机构署名:
本校为第一且通讯机构
院系归属:
药学院
摘要:
A new series of tertiary amine derivatives of chlorochalcone (4a∼4l) were designed, synthesized and evaluated for the effect on acetylcholinesterase (AChE) and buthylcholinesterase (BuChE). The results indicated that all compounds revealed moderate or potent inhibitory activity against AChE, and some possessed high selectivity for AChE over BuChE. The structure–activity investigation showed that the substituted position of chlorine significantly influenced the activity and selectivity. The alteration of tertiary amine group also leads to obvi...

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