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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.
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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.
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    Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties
    (ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2016) Secci, Daniela; Carradori, Simone; Bizzarri, Bruna; Chimenti, Paola; De Monte, Celeste; Mollica, Adriano; Rivanera, Daniela
    Pursuing our recent outcomes regarding the antifungal activity of N-substituted 1,3-thiazolidin-4-ones, we synthesized thirty-six new derivatives introducing aliphatic, cycloaliphatic and heteroaromatic moieties at N1-hydrazine connected with C2 position of the thiazolidinone nucleus and functionalizing the lactam nitrogen with differently substituted (NO2, NH2, Cl and F) benzyl groups. These compounds were tested to evaluate their minimum inhibitory concentration (MIC) against several clinical Candida spp. with respect to topical and systemic reference drugs (clotrimazole, fluconazole, ketoconazole, miconazole, tioconazole, amphotericin B). Moreover, anti-oxidant properties were also evaluated by using different protocols including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), metal chelating and phosphomolybdenum assays. Moreover, for the most active derivatives we assessed the toxicity (CC50) against Hep2 human cells in order to characterize them as multi-target agents for fungal infections. (C) 2016 Elsevier Masson SAS. All rights reserved.
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    Phytochemical Analyses and Pharmacological Screening of Neem Oil
    (ELSEVIER, 2019) Cesa, Stefania; Sisto, Francesca; Zengin, Gökhan; Scaccabarozzi, Diletta; Kokolakis, Antonios K.; Scaltrito, Maria Maddalena; Grande, Rossella; Locatelli, Marcello; Cacciagrano, Francesco; Angiolella, Letizia; Campestre, Cristina; Granese, Arianna; Chimenti, Paola; Basilico, Nicoletta
    An Italian certified Neemseed oil was characterized through the color analysis, the HPLC phenolic fingerprint and the preliminary evaluation of the cytotoxicity profile against the human macrophage (THP-1) cell line. Moreover, a wide screening of its enzyme inhibitory profile, antimicrobial activity towards Helicobacter pylori, several Candida spp. and Malassezia furfur strains and antiprotozoal activity against Plasmodium falciparum, Leishmania infantum and Leishmania tropica were performed. Neemseed oil demonstrated low toxicity and a great inhibitory efficacy against tyrosinase and lipase enzymes. Antimalarial and anti-leishmanial activities were also demonstrated, but weak or no activity was evidenced against Helicobacter pylori, Candida and Malassezia strains. Overall, these findings encourage the potential use of this natural product in some disease treatments and justify its use in traditional medicine. (c) 2018 SAAB. Published by Elsevier B.V. All rights reserved.