Structure–activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors

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成果类型：

期刊论文

作者：

Gao, Xiao-hui;Liu, Lin-bo;Liu, Hao-ran;Tang, Jing-jing;Kang, Lu;...

通讯作者：

Liu, HR;Yan, JY

作者机构：

[Gao, Xiao-hui] Changsha Med Univ, Coll Pharm, Key Lab Breeding Base Hunan Oriented Fundamental, Changsha, Hunan, Peoples R China.

[Liu, Hao-ran; Liu, HR; Liu, Lin-bo; Kang, Lu; Tang, Jing-jing] Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.

[Yan, JY; Wu, Hongnian; Yan, Jianye; Cui, Peiwu] Hunan Univ Chinese Med, Coll Pharm, Changsha, Hunan, Peoples R China.

通讯机构：

[Liu, HR ; Yan, JY ] H

Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.

Hunan Univ Chinese Med, Coll Pharm, Changsha, Hunan, Peoples R China.

语种：

英文

关键词：

acetylcholinesterase;benzamide derivative;cholinesterase;cholinesterase inhibitor;dimethylamine;picolinamide;rivastigmine;acetylcholinesterase;amide;benzamide;benzamide derivative;cholinesterase;cholinesterase inhibitor;dimethylamine;picolinamide;picolinic acid derivative;Article;biological activity;drug synthesis;enzyme kinetics;IC50;in vitro study;molecular docking;priority journal;structure activity relation;animal;chemical structure;chemistry;dose response;eel;human;metabolism;molecular model;structure activity relation;synthesis;Acetylcholinesterase;Amides;Animals;Benzamides;Butyrylcholinesterase;Cholinesterase Inhibitors;Dimethylamines;Dose-Response Relationship, Drug;Eels;Humans;Models, Molecular;Molecular Structure;Picolinic Acids;Structure-Activity Relationship

期刊：

Journal of Enzyme Inhibition and Medicinal Chemistry

ISSN：

1475-6366

年：

2018

卷：

期：

页码：

110-114

DOI：

10.1080/14756366.2017.1399885

基金类别：

The present study was financial supported by “Natural science foundation of Hu’nan province” (No. 2017JJ2050).

机构署名：

本校为通讯机构

院系归属：

药学院

摘要：

A series of benzamide and picolinamide derivatives containing dimethylamine side chain (4a–4c and 7a–7i) were synthesised and evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity in vitro. Structure–activity relationship investigation revealed that the substituted position of dimethylamine side chain markedly influenced the inhibitory activity and selectivity against AChE and BChE. In addition, it seemed that the bioactivity of picolinamide amide derivatives was stronger than that of benzamide deriva...

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Structure–activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors

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