Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease
Identifikátory výsledku
Kód výsledku v 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>
Výsledek na webu
<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>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease
Popis výsledku v původním jazyce
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.
Název v anglickém jazyce
Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease
Popis výsledku anglicky
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.
Klasifikace
Druh
J<sub>imp</sub> - Článek v periodiku v databázi Web of Science
CEP obor
—
OECD FORD obor
30108 - Toxicology
Návaznosti výsledku
Projekt
—
Návaznosti
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Ostatní
Rok uplatnění
2019
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
International journal of molecular sciences
ISSN
1661-6596
e-ISSN
—
Svazek periodika
20
Číslo periodika v rámci svazku
16
Stát vydavatele periodika
CH - Švýcarská konfederace
Počet stran výsledku
15
Strana od-do
"Article Number: 3944"
Kód UT WoS článku
000484411100101
EID výsledku v databázi Scopus
2-s2.0-85071584421