Tacrine – benzothiazoles: novel class of potential multitarget anti-Alzheimer's drugs dealing with cholinergic, amyloid and mitochondrial systems

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68378271%3A_____%2F21%3A00561212" target="_blank" >RIV/68378271:_____/21:00561212 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/21:10421137 RIV/00216208:11150/21:10421137 RIV/00216208:11160/21:10421137
Result on the web
<a href="https://doi.org/10.1016/j.bioorg.2020.104596" target="_blank" >https://doi.org/10.1016/j.bioorg.2020.104596</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>

Result language
angličtina
Original language name
Tacrine – benzothiazoles: novel class of potential multitarget anti-Alzheimer's 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.n
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10306 - Optics (including laser optics and quantum optics)

Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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