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    Design, synthesis, and biological evaluation of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives as novel acetylcholinesterase inhibitors
    ARKIVOC (2009)
    Sijie LiuAi‐Hong YangZhe JinEr-Fang HuangDavid Chi Cheong WanHuangquan LinChun Hu
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    Abstract:
    The docking study on a novel series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives with acetylcholinesterase from Torpedo californica has demonstrated that the ligands bind to the dualsite of the enzyme.The synthesis and characterization of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives was described.The crystal structure of 6-benzyl-3-{4-[2-(1-piperidinyl)-2oxoethoxy]phenyl}thiazolo[3,2-b]-1,2,4-triazin-7-one has been characterized by X-ray diffraction.All target compounds have been screened for their efficacy as acetylcholinesterase inhibitor.The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as a reference against targets.Most of the target compounds exhibit more than 50% inhibition at 10 µM.Some derivatives showed good inhibition against AChE.The preliminary structure-activity relationships were discussed.
    Topics:
    Synthesis and Characterization of Heterocyclic Compounds
    Synthesis and Reactivity of Heterocycles
    Synthesis and biological activity
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