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dc.contributor.authorGuglielmi, Paolo
dc.contributor.authorPetzer, Anél
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorSecci, Danela
dc.contributor.authorBagetta, Donatella
dc.date.accessioned2019-09-06T08:43:33Z
dc.date.available2019-09-06T08:43:33Z
dc.date.issued2019
dc.identifier.citationGuglielmi, P. et al. 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. [https://doi.org/10.1080/14756366.2019.1653864]en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/33286
dc.identifier.urihttps://www.tandfonline.com/doi/full/10.1080/14756366.2019.1653864
dc.identifier.urihttps://doi.org/10.1080/14756366.2019.1653864
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 developeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francisen_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
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus


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