4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis

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dc.authorid0000-0002-8698-9440
dc.authorid0000-0002-5165-6013
dc.contributor.authorSecci, Daniela
dc.contributor.authorCarradori, Simone
dc.contributor.authorPetzer, Anel
dc.contributor.authorGuglielmi, Paolo
dc.contributor.authorD'Ascenzio, Melissa
dc.contributor.authorChimenti, Paola
dc.contributor.authorBagetta, Donatella
dc.contributor.authorAlcaro, Stefano
dc.contributor.authorZengin, Gökhan
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorOrtuso, Francesco
dc.date.accessioned2020-03-26T20:12:13Z
dc.date.available2020-03-26T20:12:13Z
dc.date.issued2019
dc.departmentSelçuk Üniversitesi, Fen Fakültesi, Biyoloji Bölümü.en_US
dc.description.abstractA new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure-activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.en_US
dc.description.sponsorshipProgetto di Ricerca Ateneo La Sapienza (Italy) [C26A14AC5L]; POR FESR LAZIO 2014/2020 - REGIONE LAZIO - Avviso pubblico LIFE 2020en_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.en_US
dc.identifier.citationSecci, D., Carradori, S., Petzer, A., Guglielmi, P., D’Ascenzio, M., Chimenti, P., Bagetta, D., Alcaro, S., Zengin, G., Petzer, J. P., Ortuso, F. (2019). 4-(3-Nitrophenyl)Thiazol-2-Ylhydrazone Derivatives as Antioxidants and Selective Hmao-B İnhibitors: Synthesis, Biological Activity and Computational Analysis, 34(1), 597-612.
dc.identifier.doi10.1080/14756366.2019.1571272en_US
dc.identifier.endpage612en_US
dc.identifier.issn1475-6366en_US
dc.identifier.issn1475-6374en_US
dc.identifier.issue1en_US
dc.identifier.pmid30727777en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage597en_US
dc.identifier.urihttps://dx.doi.org/10.1080/14756366.2019.1571272
dc.identifier.urihttps://hdl.handle.net/20.500.12395/37384
dc.identifier.volume34en_US
dc.identifier.wosWOS:000457961800001en_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.subject(Thiazol-2-yl)hydrazone derivativesen_US
dc.subjectAlzheimer's diseaseen_US
dc.subjectParkinson's diseaseen_US
dc.subjectSelectiveen_US
dc.subjectMonoamine oxidaseen_US
dc.subjectInhibitoren_US
dc.subjectAntioxidantsen_US
dc.subjectMolecular modellingen_US
dc.title4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysisen_US
dc.typeArticleen_US

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