Synthesis and in vitro antifungal activity of 2-aryl-5-phenylsulfonyl-1,3,4-thiadiazole derivatives

The synthesis and antifungal activity of a series of 2-nitroaryl-5-phenylsu lfonyl-1,3,4-thiadiazoles (5a-e) are described. The in vitro antifungal act ivity of the compounds was determined against a variety of fungal strains i n comparison to miconazole (CAS 22916-47-8) and fluconazole (CAS 86386-73-4 ). Two derivatives (5d, 5e) showed high activity against Candida albicans a nd Candida spp. having MIC values ranging from 0.048-3.12 mu g/ml, providin g higher potencies than the reference drug fluconazole. Compound 5a also sh owed high activity against Cryptococcus neoformans (MIC < 0.048 mu g/ml). T he activity of this compound against Aspergillus niger and Aspergillus fumi gatus was moderate (MIC = 1.56-6.25 mu g/ml), while fluconazole was inactiv e. Moreover, the nitroimidazole derivative 5d possessed good activity again st most fungal strains in comparison to fluconazole.