[Synthesis and antifungal activities of 1-(2-[(substituted-phenyl) methyl]thio)-2-(2,4-difluorophenyl)ethyl-1H-1,2,4-triazoles].
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.
Zhou
Y J
YJ
Department of Medicinal Chemistry, College of Pharmacy, Second Military Medical University, Shanghai 200433.
Zhang
W N
WN
Lu
J G
JG
Li
K
K
Zhu
J
J
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D003454:Cryptococcus / Q000187:drug effects; D004821:Epidermophyton / Q000187:drug effects; D007093:Imidazoles / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013175:Sporothrix / Q000187:drug effects; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000935:Antifungal Agents; D007093:Imidazoles; D014230:Triazoles; C033308:sulconazole