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  • Design, synthesis and biological evaluation of 1-benzylamino-2-hydroxyalkyl derivatives as new potential disease-modifying multifunctional anti-Alzheimer's agents [Elektronski vir]
    Panek, Dawid ...
    The multitarget approach is a promising paradigm in drug discovery, potentially leading to new treatment options for complex disorders, such as Alzheimer's disease. Herein, we present the discovery ... of a unique series of 1-benzylamino-2-hydroxyalkyl derivatives combining inhibitory activity against butyrylcholinesterase, beta-secretase, beta-amyloid and tau protein aggregation, all related to mechanisms which underpin Alzheimer's disease. Notably, diphenylpropylamine derivative 10 showed balanced activity against both disease-modifying targets beta inhibition of beta-secretase (IC50 hBACE-1 = 41.60 microM), inhibition of amyloid beta aggregation (IC50 Abeta = 3.09 microM), inhibition of tau aggregation (55% at 10 microM), as well as against symptomatic targets: butyrylcholinesterase inhibition (IC50 hBuChE = 7.22 microM). It might represent an encouraging starting point for development of multifunctional disease-modifying anti-Alzheimer's agents.
    Source: ACS chemical neuroscience. - ISSN 1948-7193 (Vol. 9, issue 5, 2018, str. 1074-1094)
    Type of material - e-article
    Publish date - 2018
    Language - english
    COBISS.SI-ID - 4465009

    Link(s):

    http://pubs.acs.org/doi/10.1021/acschemneuro.7b00461
    DOI

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