Yazar "Alcaro, Stefano" seçeneğine göre listele

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  • Küçük Resim
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    4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
    (TAYLOR & FRANCIS LTD, 2019) Secci, Daniela; Carradori, Simone; Petzer, Anel; Guglielmi, Paolo; D'Ascenzio, Melissa; Chimenti, Paola; Bagetta, Donatella; Alcaro, Stefano; Zengin, Gökhan; Petzer, Jacobus P.; Ortuso, Francesco
    A 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.
  • Küçük Resim
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    Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity
    (TAYLOR & FRANCIS LTD, 2019) Guglielmi, Paolo; Secci, Daniela; Petzer, Ariel; Bagetta, Donatella; Chimenti, Paola; Rotondi, Giulia; Ferrante, Claudio; Recinellae, Lucia; Leonee, Sheila; Alcaro, Stefano; Zengin, Gökhan; Petzer, Jacobus P.; Ortusoc, Francesco; Carradorie, Simone
    A 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.