SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF-1-2-(-N-METHYL-N-SUBSTITUTED-BENZYL)AMINO-2-(2,4-DIFLUOROPHENYL) ETHYL-1H-1,2,4-TRIAZOLES

AIM: To study the synthesis and antifungal activities of 1-2-(Nmethyl-Nsubstituted-benzyl)amino-2-(2,4 difluorophenyl)ethyl-1H-1,2,4-triazoles. METHODS: Key intermediate were prepared by Friedel-Crafts reaction, triazolyl alkylation, ketimine reduction and Leuckart reaction. The title compounds were synthesised by Nalkylation. Antifungal activities in vitro were measured by the two times dilution method. RESULTS: Twentythree 1-2-(Nmethyl-Nsubstituted-benzyl)amino-2-(2,4-difluorophenyl)ethyl-1H-1,2,4-triazoles were synthesised and first reported. All the title compounds exhibited activities against eight fungi. Many of them showed more potent antifungal activities than butenafine against Candida albicans and Candida parapsilosis. The antifungal activities of compounds 1,2,6,13,14 and 19 are 8～32 times more active than econazole against Candida albicans.Compounds 2 and 4 are 4 and 8 times more active than butenafine and 64 and 128 times more than econazole against Cryptococcus neoformans respectively. All the compounds showed equal or more potent activity against Microsporum caniso compared with econazole. CONCLUSION: Some title compounds showed strong antifungal activities and should be studied further.