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Design, synthesis, in vitro evaluation of a new pyrrolo[1,2-a]thiazolo[5,4-d]pyrimidinone derivatives as cholinesterase inhibitors against Alzheimer's disease

文献类型：期刊论文

作者Zeng, Yan2,3; Nie, Lifei2; Liu, Liu2; Niu, Chao2,3; Li, Yi2,3; Bozorov, Khurshed1,2; Zhao, Jiangyu2,3; Shen, Jingshan2,4; Aisa, Haji Akber2,3
刊名JOURNAL OF HETEROCYCLIC CHEMISTRY
出版日期2022-02-05
页码16
ISSN号0022-152X
DOI10.1002/jhet.4452
通讯作者Aisa, Haji Akber(haji@ms.xjb.ac.cn)
英文摘要A novel of 40 pyrrolo[1,2-a]thiazolo[5,4-d]pyrimidinone derivatives were designed and synthesized as cholinesterase inhibitor agents. The in vitro enzyme assays proved that most of the compounds effectively inhibited cholinesterases in the micromolar range with little cytotoxicity. Compound G15 exhibited the best inhibitory activity against acetylcholinesterase with an IC50 of 2.69 +/- 0.17 mu M. Kinetic analysis and molecular modeling testified the competitive inhibition manner of G15 was more likely to bind to the active center of acetylcholinesterase. Thus, compound G15 can be considered as promising lead compounds or candidates for the development of novel drugs against Alzheimer's disease.
WOS关键词NITROGEN-BRIDGEHEAD COMPOUNDS ; BIOLOGICAL EVALUATION ; ACETYLCHOLINESTERASE INHIBITORS ; DEOXYVASICINONE DERIVATIVES ; ACHE INHIBITORS ; POTENTIAL USE ; DISCOVERY ; BUTYRYLCHOLINESTERASE ; ALKALOIDS ; BINDING
资助项目National Key R&D Program of China[2020YFE0205600] ; West Light Foundation of The Chinese Academy of Sciences[2018-XBQNXZ-B-004] ; West Light Foundation of The Chinese Academy of Sciences[2018-XBYJRC-001]
WOS研究方向Chemistry
语种英语
出版者WILEY
WOS记录号WOS:000751360900001
源URL[http://119.78.100.183/handle/2S10ELR8/300152]  
专题中国科学院上海药物研究所
通讯作者Aisa, Haji Akber
作者单位1.Samarkand State Univ, Fac Chem, Samarkand, Uzbekistan
2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China
3.Univ Chinese Acad Sci, Beijing, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai, Peoples R China
推荐引用方式
GB/T 7714		 Zeng, Yan,Nie, Lifei,Liu, Liu,et al. Design, synthesis, in vitro evaluation of a new pyrrolo[1,2-a]thiazolo[5,4-d]pyrimidinone derivatives as cholinesterase inhibitors against Alzheimer's disease[J]. JOURNAL OF HETEROCYCLIC CHEMISTRY,2022:16.
APA Zeng, Yan.,Nie, Lifei.,Liu, Liu.,Niu, Chao.,Li, Yi.,...&Aisa, Haji Akber.(2022).Design, synthesis, in vitro evaluation of a new pyrrolo[1,2-a]thiazolo[5,4-d]pyrimidinone derivatives as cholinesterase inhibitors against Alzheimer's disease.JOURNAL OF HETEROCYCLIC CHEMISTRY,16.
MLA Zeng, Yan,et al."Design, synthesis, in vitro evaluation of a new pyrrolo[1,2-a]thiazolo[5,4-d]pyrimidinone derivatives as cholinesterase inhibitors against Alzheimer's disease".JOURNAL OF HETEROCYCLIC CHEMISTRY (2022):16.

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来源：上海药物研究所

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