Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-(N-isoproyl-N-substituted amino)-2-propanols

Objective:Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole.Methods: A isopropyl and substituted amino group were introduced and a series of title compounds were synthesized.All of them were confirmed by MS,1H-NMR,et al.The antifungal activities were also evaluated against the eight common pathogenic fungi.Results:Fifteen compounds were synthesized.All title compounds exhibited activity against fungi tested to some extent.Compounds(6c),(6d),(6e),(6f) and(6g) exhibited strong antifungal activities against eight test fungi comparable to the control drug itraconazole except Aspergillus fumigatus.Conclusion:A benzyl moiety with a group of shorter length substituted on 4-position is required for high activity.