Triazole derivatives are the major chemical group of antifungal azole derivatives. Nowadays, the most frequently used triazoles are fluconazole and itraconazole. They posses a broad spectrum of antifungal activity and reduced toxicity when compared with the other antifungals. In this study, we aimed the synthesis of new 1,2,4-triazole derivatives as novel antifungal agents. The reaction of propionic acid hydrazides with various aryl/alkyl isothiocyanates gave thiosemicarbazides which furnished the mercaptotriazoles by alkali cyclization. The 4-phenyl/cyclohexyl-5-(l-phenoxyethyl)-3- [(3,5-diaryl-2-pyrazolin-l-yl)acetyl]thio-4H-l,2,4-triazole derivatives were synthesized by reacting the mercaptotriazoles with l-(2-chloroacetyl)-3,5-diaryl-2-pyrazoline. The chemical structures of the compounds were elucidated by IR, 'H-NMR, FAB-MS spectral data and elemental analysis. Their antifungal activities against Candida albicans (two strains), Candida glabrata, Candida tropicalis, Candida krusei , Candida utilis, Geotrichum candidum were investigated. The results showed that some of the compounds have strong antifungal activity.
Keywords: Triazole, Pyrazoline, Antifungal activity