2004•Zhongguo yaowu huaxue zazhiRequires access

Synthesis and antifungal activity of triazole derivatives

Hongbing Zhao

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Abstract

Aim To study the effect of the triazole derivatives from introducing nitrogen containing a side chain of antifungal activity.Methods Twenty-two title compounds were synthesized and confirmed by elementary analysis, 1H-NMR and IR spectra.MIC_ 80 of all the title compounds were determined using the RPMI1640 test medium.Results The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities.Compound Ⅱ_ 17 showed equal or more potent activities when compared with ketoconazole and were markedly superior to fluconazole.Conclusion Proper lipid/water distribition coefficient may be important to the influence of antifungal activities for the title compounds in vitro .

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Aim To study the effect of the triazole derivatives from introducing nitrogen containing a side chain of antifungal activity.Methods Twenty-two title compounds were synthesized and confirmed by elementary analysis, 1H-NMR and IR spectra.MIC_ 80 of all the title compounds were determined using the RPMI1640 test medium.Results The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities.Compound Ⅱ_ 17 showed equal or more potent activities when compared with ketoconazole and were markedly superior to fluconazole.Conclusion Proper lipid/water distribition coefficient may be important to the influence of antifungal activities for the title compounds in vitro .

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Available abstract

Aim To study the effect of the triazole derivatives from introducing nitrogen containing a side chain of antifungal activity.Methods Twenty-two title compounds were synthesized and confirmed by elementary analysis, 1H-NMR and IR spectra.MIC_ 80 of all the title compounds were determined using the RPMI1640 test medium.Results The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities.Compound Ⅱ_ 17 showed equal or more potent activities when compared with ketoconazole and were markedly superior to fluconazole.Conclusion Proper lipid/water distribition coefficient may be important to the influence of antifungal activities for the title compounds in vitro .

Key concepts: Ketoconazole, Chemistry, Antifungal, Fluconazole, Triazole, Proton NMR, In vitro, Minimum inhibitory concentration

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