Thiazolidinsone derivatives bearing sulfonamide group as potential antimicrobial agents: biological and in silico evaluation.

Abstract

Infectious diseases remain a significant public health threat with global socio-economic impacts. The increasing resistance to current antimicrobial therapies highlights the urgent need for new treatments with novel mechanisms of action. This study investigates the antimicrobial potential of two series of thiazolidinone derivatives, previously synthesized, using conventional and microwave-assisted methods. Antimicrobial activity was evaluated using the microdilution method, and the ability to inhibit Candida albicans biofilm formation was assessed. AutoDock 4.2® software was employed to explore potential molecular targets in bacteria and fungi. Series A compounds exhibited moderate to weak antibacterial activity (MIC/MBC: 1.50-6.00/3.00-12.0 mg/mL), with A8 being the most active (MIC: 1.5-6.0 mg/mL). Series B showed stronger antibacterial effects (MIC/MBC: 0.37-3.00/1.50-6.00 mg/mL), particularly compound B4 (MIC: 0.375-1.50 mg/mL). For antifungal activity, series A compounds were more effective (MIC/MFC: 0.37-3.00/0.75-6.00 mg/mL), with A3 showing the best results (MIC: 0.37-0.75 mg/mL). Series A also inhibited C. albicans biofilm formation, with A2 (57.7%), A4 (65.44%), and A8 (50.35%) outperforming ketoconazole (47%). These findings highlight A2, A4, and A8 as promising candidates for antibiofilm development, with A8 emerging as a lead compound due to its dual antibacterial and antifungal potency.