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  • [Synthesis and antifungal activities of 1-(2-[(substituted-phenyl) methyl]thio)-2-(2,4-difluorophenyl)ethyl-1H-1,2,4-triazoles].

[Synthesis and antifungal activities of 1-(2-[(substituted-phenyl) methyl]thio)-2-(2,4-difluorophenyl)ethyl-1H-1,2,4-triazoles].

Yao xue xue bao = Acta pharmaceutica Sinica (2001-10-13)
Y J Zhou, W N Zhang, J G Lu, K Li, J Zhu
ABSTRACT

Twenty-one 1-[2-[[(substituted-phenyl) methyl] thio]-2-(2, 4-difluorophenyl) ethyl]-1H-1,2,4-triazoles were synthesized and 19 compounds are reported for the first time. Results of biological tests in vitro showed that the antifungal activities of all title compounds were better than or comparable to the activities of fluconazole. The antifungal activities of compounds 1-7 and 11-17 were better than or comparable to the activities of sulconazole. Compounds 1, 2 and 5 were 512 times more active than sulconazole against epidermophyton floccosum; compound 5 was 32 times more active against Candida albicans, compound 2 was 32 times more active against Sporotrichum schenckii; compounds 2 and 14 were shown to be 64 and 32 times more active against Cryptococcus neoformans; compounds 1 and 5 were 16 times more active against Aspergillus fumigatus.