DESIGN AND SYNTHESIS OF SOME NEW ARYLAZOLE BASED DERIVATIVES FOR PHARMACOLOGICAL TESTING

The urgent need for innovative therapeutic solutions is highlighted by the recent rise in antimicrobial resistance. This study describes the design, synthesis, and biological evaluation of a novel series of phenyl thiazolidinone derivatives aimed at combating MRSA. The chemical structures of these compounds were precisely characterized using spectroscopic techniques. The results of comprehensive antibacterial assessments, including agar well diffusion, minimum inhibitory concentration (MIC), and time-kill kinetics, demonstrated selected compounds 4b and 4c, exhibit potent activity against MRSA ATCC 43300. Compound 4c, with an MIC of 31.25 µg/mL, emerged as the most effective, displaying bactericidal properties and a notable capacity to disrupt mature MRSA biofilms by approximately 51% at 4× MIC. Structure-activity relationship (SAR) analysis revealed that electron-donating substituents at the C4 position significantly enhance antibacterial efficacy. These findings introduce promising chemical scaffolds with dual antibacterial and antibiofilm capabilities, offering critical insights for the future development of thiazolidinone-based anti-MRSA agents.