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Tacrine - Benzothiazoles: Novel class of potential multitarget anti-Alzheimets drugs dealing with cholinergic, amyloid and mitochondrial systems

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F21%3A43920493" target="_blank" >RIV/00023752:_____/21:43920493 - isvavai.cz</a>

  • Alternative codes found

    RIV/60162694:G44__/21:00556798

  • Result on the web

    <a href="https://www.sciencedirect.com/science/article/pii/S0045206820318940?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0045206820318940?via%3Dihub</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.bioorg.2020.104596" target="_blank" >10.1016/j.bioorg.2020.104596</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Tacrine - Benzothiazoles: Novel class of potential multitarget anti-Alzheimets drugs dealing with cholinergic, amyloid and mitochondrial systems

  • Original language description

    A series of tacrine – benzothiazole hybrids incorporate inhibitors of acetylcholinesterase (AChE), amyloid β (Aβ) aggregation and mitochondrial enzyme ABAD, whose interaction with Aβ leads to mitochondrial dysfunction, into a single molecule. In vitro, several of 25 final compounds exerted excellent anti-AChE properties and interesting capabilities to block Aβ aggregation. The best derivative of the series could be considered 10w that was found to be highly potent and selective towards AChE with the IC50 value in nanomolar range. Moreover, the same drug candidate exerted absolutely the best results of the series against ABAD, decreasing its activity by 23% at 100 µM concentration. Regarding the cytotoxicity profile of highlighted compound, it roughly matched that of its parent compound – 6-chlorotacrine. Finally, 10w was forwarded for in vivo scopolamine-induced amnesia experiment consisting of Morris Water Maze test, where it demonstrated mild procognitive effect. Taking into account all in vitro and in vivo data, highlighted derivative 10w could be considered as the lead structure worthy of further investigation.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    30210 - Clinical neurology

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Others

  • Publication year

    2021

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Bioorganic Chemistry

  • ISSN

    0045-2068

  • e-ISSN

  • Volume of the periodical

    107

  • Issue of the periodical within the volume

    February

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    19

  • Pages from-to

    104596

  • UT code for WoS article

    000618104800008

  • EID of the result in the Scopus database

    2-s2.0-85099004986