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Morphing cholinesterase inhibitor amiridine into multipotent drugs for the\ntreatment of Alzheimer’s disease

  1. 1.
    0584241 - ÚEM 2025 RIV NL eng J - Článek v odborném periodiku
    Mezeiová, E. - Prchal, L. - Hrabinová, M. - Mucková, L. - Pulkrabková, L. - Soukup, O. - Misiachna, Anna - Janoušek, J. - Fibigar, J. - Kučera, T. - Horák, Martin - Makhaeva, G.F. - Korabecný, J.
    Morphing cholinesterase inhibitor amiridine into multipotent drugs for the
    treatment of Alzheimer’s disease.
    Biomedicine & Pharmacotherapy. Roč. 173, april. (2024), č. článku 116399. ISSN 0753-3322. E-ISSN 1950-6007
    Grant CEP: GA ČR(CZ) GA22-24384S; GA MŠMT(CZ) EH22_008/0004562
    Institucionální podpora: RVO:68378041
    Klíčová slova: amiridine * acetylcholinesterase * antioxidant capacity * butyrylcholinesterase * multi-target directed ligands * NMDA receptors
    Obor OECD: Neurosciences (including psychophysiology
    Impakt faktor: 7.5, rok: 2022
    Způsob publikování: Open access
    https://www.sciencedirect.com/science/article/pii/S075333222400283X?via%3Dihub

    The search for novel drugs to address the medical needs of Alzheimer’s disease (AD) is an ongoing process relying
    on the discovery of disease-modifying agents. Given the complexity of the disease, such an aim can be pursued by
    developing so-called multi-target directed ligands (MTDLs) that will impact the disease pathophysiology more
    comprehensively. Herewith, we contemplated the therapeutic efficacy of an amiridine drug acting as a cholinesterase
    inhibitor by converting it into a novel class of novel MTDLs. Applying the linking approach, we have
    paired amiridine as a core building block with memantine/adamantylamine, trolox, and substituted benzothiazole
    moieties to generate novel MTDLs endowed with additional properties like N-methyl-D-aspartate
    (NMDA) receptor affinity, antioxidant capacity, and anti-amyloid properties, respectively. The top-ranked
    amiridine-based compound 5d was also inspected by in silico to reveal the butyrylcholinesterase binding differences
    with its close structural analogue 5b. Our study provides insight into the discovery of novel amiridinebased
    drugs by broadening their target-engaged profile from cholinesterase inhibitors towards MTDLs with
    potential implications in AD therapy.
    Trvalý link: https://hdl.handle.net/11104/0352201

     
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