Romanian Society of Pharmaceutical Sciences

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MICROWAVE ASSISTED SYNTHESIS OF 3,5-DISUBSTITUTED THIAZOLIDINE-2,4-DIONES WITH ANTIFUNGAL ACTIVITY. DESIGN, SYNTHESIS, VIRTUAL AND IN VITRO ANTIFUNGAL SCREENING

GABRIEL MARC1, IOANA IONUȚ1*, ADRIAN PÎRNĂU2, LAURIAN VLASE3, DAN CRISTIAN VODNAR4, MIHAELA DUMA5, BRÎNDUȘA TIPERCIUC1, OVIDIU ONIGA1

1.“Iuliu Hațieganu” University of Medicine and Pharmacy, Department of Pharmaceutical Chemistry, 41 Victor Babeș Street, RO-400012, Cluj-Napoca, Romania
2.National Institute for Research and Development of Isotopic and Molecular Technologies, RO-400293, Cluj-Napoca, Romania
3.“Iuliu Hațieganu” University of Medicine and Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 41 Victor Babeș Street, RO-400012, Cluj-Napoca, Romania
4.University of Agricultural Sciences and Veterinary Medicine, Department of Food Science, 3-5 Mănăștur Street, RO-400372, Cluj-Napoca, Romania
5.State Veterinary Laboratory for Animal Health and Food Safety, 1 Piața Mărăști Street, RO-400572, Cluj-Napoca, Romania

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Twelve thiazolidin-2,4-diones were obtained by microwave assisted synthesis. All the synthesized compounds were physico-chemically characterized and the IR (infrared spectra), 1H-NMR (proton nuclear magnetic resonance) and MS (mass spectrometry) data were consistent with the assigned structures. All the compounds were tested for their in vitro antifungal properties against several strains of Candida and all compounds exhibited efficient anti-Candida activity. Molecular docking studies were performed to investigate the mode of action towards the fungal lanosterol 14α-demethylase. The results of the in vitro antifungal activity screening and docking study revealed that the synthesized compounds are potential anti-Candida agents that might act by inhibiting the fungal lanosterol 14α-demethylase and can be further optimized and developed as lead compounds.