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

• DOI: 10.1016/j.ejmech.2016.04.012
• Publication Date: 2016-04-10T03:09:53Z
• Authors: Daniela Secci; Simone Carradori; Bruna Bizzarri; Paola Chimenti; Celeste De Monte; Adriano Mollica; Daniela Rivanera; Alessandra Zicari; Emanuela Mari; Gokhan Zengin; Abdurrahman Aktumsek
• Keywords: 0301 basic medicine; Antifungal Agents; Anti-Candida activity; Cytotoxicity; N-benzyl-4-thiazolidinones; Anti-oxidant agents; Metal chelating agents; Hep G2 Cells; Microbial Sensitivity Tests; Antioxidants; 3. Good health; Anti-Candida activity; Anti-oxidant agents; Cytotoxicity; Metal chelating agents; N-benzyl-4-thiazolidinones; 03 medical and health sciences; Toxicity Tests; Humans; Thiazolidines; Candida; Chelating Agents

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.