Synthesis And Antifungal Activity Of 1-(1H-1,2,4-Triazole-1-yl)-2-(t-Butyl)-3-Substituted-2-Propanols

In an effort to search for novel, less toxic and broad spectrum antimycotics, twenty 1-(1H-1,2,4 - triazole- 1 - yl) -2- (t-butyl) - 3 - substituted - 2 - propanols were designed and synthesized according to the antifungal mechanism and structure-activity relationship of the triazolanol compounds, nineteen were reported firstly. All intermediates and title compounds were ascertained by means of element analysis and ~1HNMR, parts of which ascertained by MS and IR.MICs of all title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards(NCCLS) using RPMI1640 test medium. The same six fungi were used in two group: Candida albicans ATCC76615, Cryptococcus neoformans ATCC32609, Candida tropicalis, Candida parapsilosis, Fonsecaea compacta and Trichophyton rubrum, the first four of which were deep fungi. The other two fungi were Aspergillus fumigatus, Microsporum lauosum and Trichophyton tonsurans , Trichophyton verrucosum respectively.The results of preliminary antifungal test showed that all title compounds exhibited potent antifungal activities to a certain extent. Some compounds' antifungal activity approximated to Fluconazole. One of the compound with 4- (3, 4-bichlorobenzyl) piperazine showed higher activity than Fluconazole, which were worth further studied. The structure-activity relationship of the title compounds was also discussed, which will be good for further study of looking for novel antifungal drugs.