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Discovery of potent and selective acetylcholinesterase (AChE) inhibitors: acacetin 7-O-methyl ether Mannich base derivatives synthesised from easy access natural product naringin

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成果类型:
期刊论文
作者:
Liu, Hao-ran;Men, Xue;Gao, Xiao-hui;Liu, Lin-bo;Fan, Hao-qun;...
通讯作者:
Wang, Qiu-an
作者机构:
[Liu, Hao-ran; Liu, Lin-bo; Fan, Hao-qun; Wang, Qiu-an; Men, Xue] Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.
[Xia, Xin-hua; Gao, Xiao-hui] Hunan Univ Chinese Med, Coll Pharm, Changsha, Hunan, Peoples R China.
通讯机构:
[Wang, Qiu-an] H
Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.
语种:
英文
关键词:
Alzheimer's diseases;Mannich base;Naringin;acetylcholinesterase inhibitors;molecular docking
期刊:
Natural Product Research
ISSN:
1478-6419
年:
2018
卷:
32
期:
6
页码:
743-747
基金类别:
Innovative Investigation funds for graduated students of Hu'nan province [CX2015B324]; Natural Science Foundation of Hu'nan ProvinceNatural Science Foundation of Hunan Province [2017JJ2050]
机构署名:
本校为其他机构
院系归属:
药学院
摘要:
Naringin, as a component universal existing in the peel of some fruits or medicinal plants, was usually selected as the material to synthesise bioactive derivates since it was easy to gain with low cost. In present investigation, eight new acacetin-7-O-methyl ether Mannich base derivatives (1–8) were synthesised from naringin. The bioactivity evaluation revealed that most of them exhibited moderate or potent acetylcholinesterase (AChE) inhibitory activity. Among them, compound 7 (IC50 for AChE = 0.82 ± 0.08 μmol•L−1, IC50 for BuChE = 46.30...

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