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KMID : 0043320100330101641
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Archives of Pharmacal Research
2010 Volume.33 No. 10 p.1641 ~ p.1649
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Synthesis and biological evaluation of 3,6-diaryl-7H-thiazolo[3,2-b] [1,2,4]triazin-7-one derivatives as acetylcholinesterase inhibitors
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Jin Zhe
Yang Liu
Liu Si Jie
Wang Jian
Li Shuo
Lin Huang Quan
Wan David Chi Cheong
Hu Chun
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Abstract
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Acetylcholinesterase (AChE) inhibitors played an important role in developing a cure for Alzheimer’ s disease. In order to study on the influence of modifications at different groups and side chains on the AChE inhibitory ability and the active sites of 7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives, fourteen 3,6-diaryl-7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives were designed and synthesized. The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control drug. Most of the target compounds exhibited more than 50% inhibition at 10 μM. Some target compounds showed strong inhibition against AChE. The molecular fields analysis and preliminary structureactivity relationships are discussed.
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KEYWORD
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Acetylcholinesterase, Inhibitor, Heterocycle, Thiazole, 1, 2, 4-Triazine, Molecular docking, Molecular fields analysis
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