Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity

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dc.authorid0000-0002-0437-358X
dc.authorid0000-0002-5165-6013
dc.authorid0000-0001-6235-8161
dc.authorid0000-0002-8698-9440
dc.contributor.authorGuglielmi, Paolo
dc.contributor.authorSecci, Daniela
dc.contributor.authorPetzer, Ariel
dc.contributor.authorBagetta, Donatella
dc.contributor.authorChimenti, Paola
dc.contributor.authorRotondi, Giulia
dc.contributor.authorFerrante, Claudio
dc.contributor.authorRecinellae, Lucia
dc.contributor.authorLeonee, Sheila
dc.contributor.authorAlcaro, Stefano
dc.contributor.authorZengin, Gökhan
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorOrtusoc, Francesco
dc.contributor.authorCarradorie, Simone
dc.date.accessioned2020-03-26T20:12:42Z
dc.date.available2020-03-26T20:12:42Z
dc.date.issued2019
dc.departmentSelçuk Üniversitesi, Fen Fakültesi, Biyoloji Bölümüen_US
dc.description.abstractA series of benzo[b]thiophen-3-ols were synthesised and investigated as potential human monoamine oxidase (hMAO) inhibitors in vitro as well as ex vivo in rat cortex synaptosomes by means of evaluation of 3,4-dihydroxyphenylacetic acid/dopamine (DOPAC/DA) ratio and lactate dehydrogenase (LDH) activity. Most of these compounds possessed high selectivity for the MAO-B isoform and a discrete antioxidant and chelating potential. Molecular docking studies of all the compounds underscored potential binding site interactions suitable for MAO inhibition activity, and suggested structural requirements to further improve the activity of this scaffold by chemical modification of the aryl substituents. Starting from this heterocyclic nucleus, novel lead compounds for the treatment of neurodegenerative disease could be developed.en_US
dc.description.sponsorshipProgetto di Ricerca Ateneo La Sapienza (Italy) [2014-C26A14AC5L]; POR FESR LAZIO 2014/2020 - REGIONE LAZIO - Avviso pubblico LIFE 2020; National Research Foundation of South AfricaNational Research Foundation - South Africa [85642, 96180]en_US
dc.description.sponsorshipThis work was supported by "Progetto di Ricerca Ateneo La Sapienza 2014-C26A14AC5L" (Italy) and POR FESR LAZIO 2014/2020 - REGIONE LAZIO - Avviso pubblico LIFE 2020 (Prof. Daniela Secci). The monoamine oxidase inhibition experiments were supported by grants from the National Research Foundation of South Africa (Grant specific unique reference numbers (UID) 85642, 96180). Opinions expressed and conclusions arrived at, are those of the authors and therefore the NRF do not accept any liability in regard thereto.en_US
dc.identifier.citationGuglielmi, P., Secci, D., Petzer, A., Bagetta, D., Chimenti, P., Rotondi, G., Ferrante, C., Recinella, L.,Leone, S., Alcaro, S., Zengin, G., Petzer, J. P., Ortuso, F., Carradori, S. (2019). Benzo [b] Tiophen-3-ol Derivatives as Effective Inhibitors of Human Monoamine Oxidase: Design, Synthesis, and Biological Activity. Journal of Enzyme Inhibition and Medicinal Chemistry, 34(1), 1511-1525.
dc.identifier.doi10.1080/14756366.2019.1653864en_US
dc.identifier.endpage1525en_US
dc.identifier.issn1475-6366en_US
dc.identifier.issn1475-6374en_US
dc.identifier.issue1en_US
dc.identifier.pmid31422706en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage1511en_US
dc.identifier.urihttps://dx.doi.org/10.1080/14756366.2019.1653864
dc.identifier.urihttps://hdl.handle.net/20.500.12395/37527
dc.identifier.volume34en_US
dc.identifier.wosWOS:000481738100001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorZengin, Gökhan
dc.language.isoenen_US
dc.publisherTAYLOR & FRANCIS LTDen_US
dc.relation.ispartofJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRYen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.selcuk20240510_oaigen_US
dc.subjectMAO-B inhibitorsen_US
dc.subjectBenzothiopheneen_US
dc.subjectMolecular modellingen_US
dc.subjectRat cortex synaptosomesen_US
dc.subjectAntioxidant activityen_US
dc.subjectParkinson's diseaseen_US
dc.titleBenzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activityen_US
dc.typeArticleen_US

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