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dc.creatorJevtić, Ivana I.
dc.creatorLai, Thu Hang
dc.creatorPenjišević, Jelena
dc.creatorDukić-Stefanović, Slađana
dc.creatorAndrić, Deana
dc.creatorBrust, Peter
dc.creatorKostić-Rajačić, Slađana
dc.creatorTeodoro, Rodrigo
dc.date.accessioned2020-12-11T22:23:57Z
dc.date.available2020-12-11T22:23:57Z
dc.date.issued2020
dc.identifier.issn1420-3049
dc.identifier.urihttp://cherry.chem.bg.ac.rs/handle/123456789/4272
dc.description.abstractHerein, we report on the synthesis and pharmacological evaluation of ten novel fluorinated cinnamylpiperazines as potential monoamine oxidase B (MAO-B) ligands. The designed derivatives consist of either cinnamyl or 2-fluorocinnamyl moieties connected to 2-fluoropyridylpiperazines. The three-step synthesis starting from commercially available piperazine afforded the final products in overall yields between 9% and 29%. An in vitro competitive binding assay using l-[3H]Deprenyl as radioligand was developed and the MAO-B binding affinities of the synthesized derivatives were assessed. Docking studies revealed that the compounds 8–17 were stabilized in both MAO-B entrance and substrate cavities, thus resembling the binding pose of l-Deprenyl. Although our results revealed that the novel fluorinated cinnamylpiperazines 8–17 do not possess sufficient MAO-B binding affinity to be eligible as positron emission tomography (PET) agents, the herein developed binding assay and the insights gained within our docking studies will certainly pave the way for further development of MAO-B ligands.
dc.languageen
dc.publisherMDPI
dc.relationMinistry of Education, Science and Technological Development of the Republic of Serbia (grant No. 451-03-01732/2017-09/4).
dc.relationDeutscher Akademischer Austauschdienst (DAAD, grant No. 57391403) within the Bilateral project “Development of new fluorinated radioligands for PET imaging of monoamine oxidase B (MAO-B)”.
dc.rightsopenAccess
dc.sourceMolecules
dc.subjectcinnamic acid
dc.subjectMAO-B
dc.subjectpiperazine
dc.subjectpositron emission tomography
dc.titleNewly Synthesized Fluorinated Cinnamylpiperazines Possessing Low In Vitro MAO-B Binding
dc.typearticleen
dc.rights.licenseBY
dcterms.abstractКостић-Рајачић, Слађана; Дукић-Стефановић, Слађана; Пењишевић, Јелена; Лаи, Тху Ханг; Бруст, Петер; Теодоро, Родриго; Aндрић, Деана; Јевтић, Ивана И.;
dc.citation.volume25
dc.citation.issue21
dc.citation.spage4941
dc.identifier.wos000589372800001
dc.identifier.doi10.3390/molecules25214941
dc.citation.rankM22~
dc.type.versionpublishedVersion
dc.identifier.scopus2-s2.0-85094821384
dc.identifier.fulltexthttp://cherry.chem.bg.ac.rs/bitstream/id/26403/Newly_Synthesized_Fluorinated_pub_2020.pdf


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