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dc.creatorJevtić, Ivana
dc.creatorLai, Thu Hang
dc.creatorPenjišević, Jelena
dc.creatorDukić-Stefanović, Sladjana
dc.creatorAndrić, Deana
dc.creatorBrust, Peter
dc.creatorKostić Rajačić, Slađana
dc.creatorTeodoro, Rodrigo
dc.date.accessioned2020-12-17T14:46:21Z
dc.date.available2020-12-17T14:46:21Z
dc.date.issued2020
dc.identifier.issn1420-3049
dc.identifier.urihttps://cer.ihtm.bg.ac.rs/handle/123456789/4040
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.en
dc.publisherBasel, Switzerland : MDPIen
dc.relationMinistry of Education, Science and Technological Development of the Republic of Serbia (grant No. 451-03-01732/2017-09/4) and the Deutscher 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.sourceMoleculesen
dc.subjectMAO-B
dc.subjectpositron emission tomography
dc.subjectpiperazine
dc.subjectcinnamic acid
dc.titleNewly Synthesized Fluorinated Cinnamylpiperazines Possessing Low In Vitro MAO-B Bindingen
dc.typearticleen
dc.rights.licenseBY
dcterms.abstractЛаи, Тху Ханг; Костић Рајачић, Сладјана; Теодоро, Родриго; Бруст, Петер; Дукић-Стефановић, Сладјана; Јевтић, Ивана; Пењишевић, Јелена; Aндрић, Деана;
dc.rights.holderThe Authors
dc.citation.volume25
dc.citation.issue21
dc.citation.spage4941
dc.citation.rankM22~
dc.identifier.doi10.3390/molecules25214941
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs/bitstream/id/18530/molecules-25-04941.pdf
dc.identifier.scopus2-s2.0-85094821384
dc.identifier.wos000589372800001
dc.type.versionpublishedVersion


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