Donepezil plus chromone plus melatonin hybrids as promising agents for Alzheimer's disease therapy

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F19%3A50015421" target="_blank" >RIV/62690094:18470/19:50015421 - isvavai.cz</a>
Result on the web
<a href="https://www.tandfonline.com/doi/full/10.1080/14756366.2018.1545766" target="_blank" >https://www.tandfonline.com/doi/full/10.1080/14756366.2018.1545766</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1080/14756366.2018.1545766" target="_blank" >10.1080/14756366.2018.1545766</a>

Result language
angličtina
Original language name
Donepezil plus chromone plus melatonin hybrids as promising agents for Alzheimer's disease therapy
Original language description
We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 +/- 0.05 nM), moderate hAChE (IC50 = 1.73 +/- 0.34 mu M), hMAO A (IC50 = 2.78 +/- 0.12 mu M), and MAO B (IC50 = 21.29 +/- 3.85 mu M) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure.
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
30107 - Medicinal chemistry

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

Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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