| Literature DB >> 27100030 |
Daniela Secci1, Simone Carradori2, Bruna Bizzarri1, Paola Chimenti1, Celeste De Monte1, Adriano Mollica3, Daniela Rivanera4, Alessandra Zicari5, Emanuela Mari5, Gokhan Zengin6, Abdurrahman Aktumsek6.
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.Entities:
Keywords: Anti-Candida activity; Anti-oxidant agents; Cytotoxicity; Metal chelating agents; N-benzyl-4-thiazolidinones
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Year: 2016 PMID: 27100030 DOI: 10.1016/j.ejmech.2016.04.012
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514