Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F19%3A50015921" target="_blank" >RIV/62690094:18470/19:50015921 - isvavai.cz</a>
Result on the web
<a href="https://www.mdpi.com/1422-0067/20/16/3944/htm" target="_blank" >https://www.mdpi.com/1422-0067/20/16/3944/htm</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/ijms20163944" target="_blank" >10.3390/ijms20163944</a>

Result language
angličtina
Original language name
Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease
Original language description
Six quinoline-piperonal hybrids were synthesized and evaluated as potential drugs against Alzheimer's disease (AD). Theoretical analysis of the pharmacokinetic and toxicological properties of the compounds suggest that they present good oral bio-availability and are also capable of penetrating the blood-brain barrier, qualifying as leads for new drugs against AD. Evaluation of their inhibitory capacity against acetyl- and butyrilcholinesterases (AChE and BChE) through Ellmann's test showed that three compounds present promising results with one of them being capable of inhibiting both enzymes. Further docking studies of the six compounds synthesized helped to elucidate the main interactions that may be responsible for the inhibitory activities observed.
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
30108 - Toxicology

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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