Nitrogen-containing flavonoid and their analogs with diverse B-ring in acetylcholinesterase and butyrylcholinesterase inhibition

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成果类型：

期刊论文

作者：

Lu, Qiao-Qiao;Chen, Ya-Ming;Liu, Hao-Ran;Yan, Jian-Ye;Cui, Pei-Wu;...

通讯作者：

Liu, HR;Liu, YZ

作者机构：

[Liu, Hao-Ran; Zhang, Qian-Fan; Lu, Qiao-Qiao; Chen, Ya-Ming] Hunan Univ, Dept Chem Biol, Coll Chem & Chem Engn, Changsha, Peoples R China.

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

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

[Feng, Xing; Liu, Ying-Zi] Hunan Normal Univ, Dept Pharm, Coll Med, Changsha, Peoples R China.

[Liu, HR] Hunan Univ, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China.

通讯机构：

[Liu, HR ; Liu, YZ ] H

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

Hunan Normal Univ, Coll Med, Changsha 410013, Peoples R China.

语种：

英文

关键词：

cholinesterase inhibitors;flavonoid analog;structure-activity relationship

期刊：

Drug Development Research

ISSN：

0272-4391

年：

2020

卷：

期：

页码：

1037-1047

DOI：

10.1002/ddr.21726

基金类别：

Qiao-Qiao Lu and Ya-Ming Chen contributed equally to this work and should be regarded as co-first authors. the Grant of Department of Education of Hu'nan Province, Grant/Award Number: 18B543; the grant of Key Laboratory Breeding Base of Hu'nan Oriented Fundamental and Applied Research of Innovative Pharmaceutics, Grant/Award Number: 2016TP1029

机构署名：

本校为其他机构

院系归属：

药学院

摘要：

AbstractIn this study, a series of new flavones (2‐phenyl‐chromone), 2‐naphthyl chromone, 2‐anthryl‐chromone, or 2‐biphenyl‐chromone derivatives containing 6 or 7‐substituted tertiary amine side chain were designed, synthesized, and evaluated in acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition. The results indicated that the alteration of aromatic ring connecting to chromone scaffold brings about a significant impact on biological activity. Compared with flavones, the inhibitory activity of 2‐naphthyl chromone, 2...

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Nitrogen-containing flavonoid and their analogs with diverse B-ring in acetylcholinesterase and butyrylcholinesterase inhibition

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