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, mi- conazole, 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.

Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties / Secci, Daniela; Simone, Carradori; Bizzarri, Bruna; Chimenti, Paola; DE MONTE, Celeste; Adriano, Mollica; Rivanera, Daniela; Zicari, Alessandra; Emanuela, Mari; Gokhan, Zengin; Abdurrahman, Aktumsek. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 117:(2016), pp. 144-156. [dx.doi.org/10.1016/j.ejmech.2016.04.012.]

Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties

SECCI, DANIELA;BIZZARRI, Bruna;CHIMENTI, Paola;DE MONTE, CELESTE;RIVANERA, Daniela;ZICARI, Alessandra;
2016

Abstract

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, mi- conazole, 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.
2016
Anti-Candida activity; Anti-oxidant agents; Cytotoxicity; Metal chelating agents; N-benzyl-4-thiazolidinones
01 Pubblicazione su rivista::01a Articolo in rivista
Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties / Secci, Daniela; Simone, Carradori; Bizzarri, Bruna; Chimenti, Paola; DE MONTE, Celeste; Adriano, Mollica; Rivanera, Daniela; Zicari, Alessandra; Emanuela, Mari; Gokhan, Zengin; Abdurrahman, Aktumsek. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 117:(2016), pp. 144-156. [dx.doi.org/10.1016/j.ejmech.2016.04.012.]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/906767
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