Structure–activity relationship investigation of coumarin–chalcone hybrids with diverse side-chains as acetylcholinesterase and butyrylcholinesterase inhibitors

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成果类型：

期刊论文

作者：

Kang, Lu;Gao, Xiao-Hui;Liu, Hao-Ran;Men, Xue;Wu, Hong-Nian;...

通讯作者：

Liu, HR;Yan, JY

作者机构：

[Liu, Hao-Ran; Liu, HR; Kang, Lu; Men, Xue] Hunan Univ, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China.

[Gao, Xiao-Hui] Changsha Med Univ, Coll Pharm, Changsha 410219, Hunan, Peoples R China.

[Yan, JY; Wu, Hong-Nian; Yan, Jian-Ye; Cui, Pei-Wu] Hunan Univ Chinese Med, Coll Pharm, Changsha 410208, Hunan, Peoples R China.

[Oldfield, Eric] Univ Illinois, Dept Chem, 1209 W Calif St, Urbana, IL 61801 USA.

通讯机构：

[Liu, HR ; Yan, JY ] H

Hunan Univ, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China.

Hunan Univ Chinese Med, Coll Pharm, Changsha 410208, Hunan, Peoples R China.

语种：

英文

关键词：

Coumarin;Chalcone;Cholinesterase inhibitors;Structure-activity relationship;Tertiary amine group

期刊：

MOLECULAR DIVERSITY

ISSN：

1381-1991

年：

2018

卷：

期：

页码：

893-906

DOI：

10.1007/s11030-018-9839-y

基金类别：

Acknowledgements This work was supported by the Natural science foundation of Hu’nan Province” (Grants Nos. 2017JJ2050, 2018JJ3572) and in part by the United States Public Health Service (NIH Grant GM065307). This work was supported by the Natural science foundation of Hu?nan Province? (Grants Nos. 2017JJ2050, 2018JJ3572) and in part by the United States Public Health Service (NIH Grant GM065307).

机构署名：

本校为通讯机构

院系归属：

药学院

摘要：

Chalcones containing tertiary amine side-chains have potent activity as acetylcholinesterase (AChE) inhibitors. However, the effects of the location of the tertiary amine groups as well as of other groups on AChE and butyrylcholinesterase (BChE) activity have not been reported. Here, we report the synthesis and testing of 36 new coumarin–chalcone hybrids (5d–7j, 9d–11f, 12k–13m) against AChE and BChE. The nature and position of the chalcone substituents had major effects on inhibitory activity as well as selectivity for AChE over BChE. Comp...

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Structure–activity relationship investigation of coumarin–chalcone hybrids with diverse side-chains as acetylcholinesterase and butyrylcholinesterase inhibitors

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