Therapeutic Evaluation of Some New Synthetic N & S Heterocycles as Potential Antifungal Agents

Antifungal agents commercially in use for human mycoses target the biosynthetic pathway to ergosterol, an important component of fungal membranes. An intermediate of the ergosterol biosynthetic pathway is the cytochrome P-450 dependent 14 a-sterol demethylase (CYP51) enzyme, which catalyzes the oxidative removal of the 14 a-methyl group of lanosterol to give D14, 15 desaturated intermediates. Some triazole derivatives such as fluconazole and voriconazole exhibit antifungal activity by inhibiting the fungal CYP-51 enzyme, thereby inhibiting the synthesis of ergosterol. The emergence of multi drug resistant strains of microbes is the outcome of widespread and prolonged use of antimicrobial drug therapy. The studies directed towards the search for new, effective and safe nuclei have led to an improvement in the existing drugs by increasing their potency, duration of action and decreasing their toxic effects. This is achieved by creating new biologically active molecules through qualitative modification. 4-Thiazolidinones exhibit various biochemical activities such as antibacterial, antiviral, anti-tubercular, anticancer and antifungal etc. Present work reports the synthesis of a new series of 4thiazolidinones. Disc diffusion method was employed for in-vitro screening of the synthesized compounds against some of the fungal pathogens for their therapeutic efficacy and these values were compared to the corresponding values for fluconazole. The venture shows assuring results.