Synthesis And Antifungal Activity Of 1-(1H-1,2,4-Triazole-1-yl)-2- (2,4-Difluorophenyl)-3-Substituted-2-Propanol

Abstract According to the antifungal mechanisms and structure-activity relationships of the triazolanol compounds., twenty-six l-(lH-l,2,4-triazol-l-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols were designed and synthesized for searching of more potent, less toxic and broad spectrum antimycotics ,23 were first reported. All intermediates and title compounds were ascertained by means of element analysis and 'HNMR, 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. Eight fungi were used: Candida albicans ATCC76615, Cryptococcus neoformans ATCC32609, Candida tropicalis, Candida parapsilosis, Trichophyton rubrum, Microsp orumcani), Fonsecaea compacta and Aspergillus fumigatus. The results of preliminary antifungal test showed that all title compounds exhibited potent antifungal activities to a certain extent. Eleven compounds are more than 4 times lower than that of Fluconazole against Candida albicans in vitro, which have promising antifungal activity and further in vitro and in vivo investigations are warranted. Also the structure-activity relationship of the title compounds was discussed.