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  • 4-phenethyl-1-propargylpiperidine-derived dual inhibitors of butyrylcholinesterase and monoamine oxidase B [Elektronski vir]
    Mazej, Tjaša ...
    The multi-target-directed ligands (MTDLs) strategy is encouraged for the development of novel modulators targeting multiple pathways in the neurodegenerative cascade typical for Alzheimer's disease ... (AD). Based on the structure of an in-house irreversible monoamine oxidase B (MAO-B) inhibitor, we aimed to introduce a carbamate moiety on the aromatic ring to impart cholinesterase (ChE) inhibition, and to furnish multifunctional ligands targeting two enzymes that are intricately involved in AD pathobiology. In this study, we synthesized three dual hMAO-B/hBChE inhibitors 13-15, with compound 15 exhibiting balanced, low micromolar inhibition of hMAO-B (IC50 of 4.3 [micro]M) and hBChE (IC50 of 8.5 [micro]M). The docking studies and time-dependent inhibition of hBChE confirmed the initial expectation that the introduced carbamate moiety is responsible for covalent inhibition. Therefore, dual-acting compound 15 represents an excellent starting point for further optimization of balanced MTDLs.
    Source: Molecules [Elektronski vir]. - ISSN 1420-3049 (Vol. 26, iss. 14, 2021, str. 1-17)
    Type of material - e-article ; adult, serious
    Publish date - 2021
    Language - english
    COBISS.SI-ID - 69610499

    Link(s):

    https://www.mdpi.com/1420-3049/26/14/4118
    Repository of the University of Ljubljana – RUL
    DOI

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