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

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

  • Eur J Med Chem. 2016 Jul 19:117:144-56. doi: 10.1016/j.ejmech.2016.04.012.
Daniela Secci 1,  Simone Carradori 2,  Bruna Bizzarri 1,  Paola Chimenti 1,  Celeste De Monte 1,  Adriano Mollica 3,  Daniela Rivanera 4,  Alessandra Zicari 5,  Emanuela Mari 5,  Gokhan Zengin 6,  Abdurrahman Aktumsek 6
Affiliations

Affiliations

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
  • 2 Department of Pharmacy, "G. D'Annunzio" University of Chieti-Pescara, Via dei Vestini 31, 66100 Chieti, Italy. Electronic address: simone.carradori@unich.it.
  • 3 Department of Pharmacy, "G. D'Annunzio" University of Chieti-Pescara, Via dei Vestini 31, 66100 Chieti, Italy.
  • 4 Dipartimento di Sanità Pubblica e Malattie Infettive, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
  • 5 Dipartimento di Medicina Sperimentale, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
  • 6 Department of Biology, Science Faculty, Selcuk University, Konya, Turkey.
PMID: 27100030 DOI: 10.1016/j.ejmech.2016.04.012
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, 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.

Keywords

Anti-Candida activity; Anti-oxidant agents; Cytotoxicity; Metal chelating agents; N-benzyl-4-thiazolidinones.

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