1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-取代-2-丙醇的合成及抗真菌活性研究

１（１Ｈ１，２，４三唑１基）２（２，４二氟苯基）３取代２丙醇的合成及抗真菌活性研究张大志周廷森吴义杰刘超美麻铭川冯向庭（第二军医大学药学院，上海２００４３３）氮唑类化合物是目前抗真菌药物研究最为活跃的领域之一。该类化合物可分...

SYNTHESIS AND ANTIFUNGAL ACTIVITY OF 1-(1H-1,2,4-TRIAZOLE-1-YL)-2-(2,4-DIFLUOROPHENYL)-3-SUBSTITUTED-2-PROPANOLS

Twenty-three 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols were synthesized and evaluated for antifungal activities in vitro. The synthetic methods of the intermediates are also reported. The compounds belong to two kinds: sulfones and sulfides. All of the compounds are new. The results of preliminary antifungal test showed that most of the sulfide derivatives exhibited potent activities against six kinds of common pathogenic fungi such as Microsporum lanosum, Cryptococcus neoformans, Candida albicans, Aspergillus fumigatus, Cladosporium carrionii, and Saccharomyces torulopsis in vitro. Compounds IVe, f,i,j showed equal or more potent activities when compared with ketoconazole and were markedly superior to fluconazole. The sulfone derivatives showed lower antifungal activity.