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Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D-2 3,4-dihydroquinolin-2(1H)-one Derivatives Related to Aripiprazole

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dc.contributor.authorJůza, Radomír
dc.contributor.authorStefkova, Kristyna
dc.contributor.authorDehaen, Wim
dc.contributor.authorRandakova, Alena
dc.contributor.authorPetrasek, Tomas
dc.contributor.authorVojtechova, Iveta
dc.contributor.authorKobrlova, Tereza
dc.contributor.authorPulkrabkova, Lenka
dc.contributor.authorMuckova, Lubica
dc.contributor.authorMecava, Marko
dc.contributor.authorPrchal, Lukas
dc.contributor.authorMezeiova, Eva
dc.contributor.authorMusílek, Kamil
dc.contributor.authorSoukup, Ondrej
dc.contributor.authorKorabecny, Jan
dc.date.accessioned2025-12-05T10:26:05Z
dc.date.available2025-12-05T10:26:05Z
dc.date.issued2021
dc.description.abstractIn this pilot study, a series of new 3,4-dihydroquinolin-2(1H)-one derivatives as potential dopamine receptor D-2 (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.eng
dc.formatp. &quot;Article Number: 1262&quot;
dc.identifier.doi10.3390/biom11091262
dc.identifier.issn2218-273X
dc.identifier.obd43877969
dc.identifier.scopus2-s2.0-85113754200
dc.identifier.urihttp://hdl.handle.net/20.500.12603/1305
dc.identifier.wos000699332600001
dc.language.isoeng
dc.peerreviewedyes
dc.publicationstatuspostprint
dc.publisherMDPI-Molecular diversity preservation international
dc.relation.ispartofBiomolecules, volume 11, issue: 9eng
dc.relation.publisherversionhttps://www.mdpi.com/2218-273X/11/9/1262
dc.rights.accessOpen Access
dc.rights.licenseCC BY
dc.source.urlhttps://www.mdpi.com/2218-273X/11/9/1262
dc.subjectaripiprazoleeng
dc.subjectdopamine receptoreng
dc.subjectblood-brain barriereng
dc.subjectmolecular modeling studieseng
dc.subjectschizophreniaeng
dc.titleSynthesis and In Vitro Evaluation of Novel Dopamine Receptor D-2 3,4-dihydroquinolin-2(1H)-one Derivatives Related to Aripiprazoleeng
dc.typearticle

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