Design,Synthesis,and Biological Evaluation of 5H-Thiazolo[3,2-a]pyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors |
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| Authors: | ZHI Hui CHEN Lan-mei ZHANG Lin-lin LIU Si-jie David Chi Cheong WAN LIN Huang-quan HU Chun School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang P R China |
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| Institution: | [1]School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China [2]Department of Biochemistry, The Chinese University of Hong Kong, Hong Kong SAR, P. R. China |
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| Abstract: | Acetylcholinesterase inhibitors are the most frequently prescribed anti-Alzheimer's drugs. A series of 5H-thiazolo3,2-a]pyrimidine-6-carboxylic acid ethyl ester derivatives as the novel acetylcholinesterase inhibitors was designed based on virtual screening methods. The target compounds were synthesized with Biginelli reaction and Hantzsch-type condensation of dihydropyrimidines with substituted phenacyl chlorides,and were characterized with elemental analysis,IR,MS,1H NMR,and 13C NMR. The biological evalu... |
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| Keywords: | Acetylcholinesterase inhibitor Docking screening Heterocycle Biological activity 5H-Thiazolo[3 2-a] pyrimidine-6-carboxylic acid ethyl ester derivative |
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