Synthesis and in vitro evaluation of novel dopamine receptor D2 3,4-dihydroquinolin-2(1H)-one derivatives related to aripiprazole
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F21%3A43920664" target="_blank" >RIV/00023752:_____/21:43920664 - isvavai.cz</a>
Alternative codes found
RIV/67985823:_____/21:00546462 RIV/00179906:_____/21:10432820 RIV/62690094:18470/21:50018359 RIV/60461373:22310/21:43923454
Result on the web
<a href="https://www.mdpi.com/2218-273X/11/9/1262" target="_blank" >https://www.mdpi.com/2218-273X/11/9/1262</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/biom11091262" target="_blank" >10.3390/biom11091262</a>
Alternative languages
Result language
angličtina
Original language name
Synthesis and in vitro evaluation of novel dopamine receptor D2 3,4-dihydroquinolin-2(1H)-one derivatives related to aripiprazole
Original language description
In this pilot study, a series of new 3,4-dihydroquinolin-2(1H)-one derivatives as potential dopamine receptor D2 (D2R) modulators were synthesized and evaluated in vitro. The preliminary structure–activity relationship disclosed that compound 5e exhibited the highest D2R affinity among the newly synthesized compounds. In addition, 5e showed a very low cytotoxic profile and a high probability to cross the blood–brain barrier, which is important considering the observed affinity. However, molecular modelling simulation revealed completely different binding mode of 5e compared to USC-D301, which might be the culprit of the reduced affinity of 5e toward D2R in comparison with USC-D301.
Czech name
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Czech description
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Classification
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
10401 - Organic chemistry
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
Biomolecules
ISSN
2218-273X
e-ISSN
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Volume of the periodical
11
Issue of the periodical within the volume
9
Country of publishing house
CH - SWITZERLAND
Number of pages
18
Pages from-to
1262
UT code for WoS article
000699332600001
EID of the result in the Scopus database
2-s2.0-85113754200