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- W3164235512 abstract "AD is a progressive brain disorder. Because of the lack of remarkable single-target drugs against neurodegenerative disorders, the multitarget-directed ligand strategy has received attention as a promising therapeutic approach. Herein, we rationally designed twenty-nine hybrids of N-propargylamine-hydroxypyridinone. The designed hybrids possessed excellent iron-chelating activity (pFe3+ = 17.09-22.02) and potent monoamine oxidase B inhibitory effects. Various biological evaluations of the optimal compound 6b were performed step by step, including inhibition screening of monoamine oxidase (hMAO-B IC50 = 0.083 ± 0.001 µM, hMAO-A IC50 = 6.11 ± 0.08 µM; SI = 73.5), prediction of blood-brain barrier permeability and mouse behavioral research. All of these favorable results proved that the N-propargylamine-hydroxypyridinone scaffold is a promising structure for the discovery of multitargeted ligands for AD therapy." @default.
- W3164235512 created "2021-06-07" @default.
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- W3164235512 date "2021-08-01" @default.
- W3164235512 modified "2023-10-02" @default.
- W3164235512 title "N-Propargylamine-hydroxypyridinone hybrids as multitarget agents for the treatment of Alzheimer’s disease" @default.
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- W3164235512 doi "https://doi.org/10.1016/j.bioorg.2021.105013" @default.
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