Synthesis of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-(N-cyclopropyl-N-substituted amino)-2-propanols and its antifungal activity
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Supported by National Natural Science Foundation of China(20772153) and Youth Initiation Program of Second Military Medical University.

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    Abstract:

    Objective:To study the antifungal activity of triazole alcohols by introduction of cyclopropyl as side chain. Methods: Ten title compounds were synthesized and characterized by 1HNMR,MS spectra and element analysis. The MICs of the compounds were determined by in vitro test in 8 fungus strains. Results: The title compounds exhibited potent antifungal activities against 8 strains,especially for the deep infection ones. Some compounds had MIC80 values less than 0.125 μg·ml-1 against Candida albicans,showing an activity 4 time higher than that of fluconzole.Conclusion: The title compounds with cyclopropyl and alky substituents have antifungal activities,and the antifungal activity decreases as the alkyl side chains getting longer.

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History
  • Received:June 11,2008
  • Revised:September 01,2008
  • Adopted:September 03,2008
  • Online: November 18,2008
  • Published:
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