2006Zhongguo yaowu huaxue zazhiRequires access

Synthesis and antifungal activities of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted-piperazine)-1-yl]-2-propanols

Qiuye Wu

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Abstract

Aim To study the effect of the triazole derivatives with the side chain containing(4-substituted-piperidine)-1-yl or second amine on the antifungal activity of triazole compounds.Methods Nine title compounds were synthesized and determined by the elementary analysis,()~1H-NMR and IR spectra.The MICs of all the title compounds were determined by the method recommended by the national committee for clinical laboratory standards(NCCLS)using the RPMI 1640 test medium.Results All of the title compounds displayed potent antifungal activities to some extent.The activity of the two compounds 4,5 were more than 4 times as high as that of fluconazole and itraconazole against Candida albicans in vitro.Conclusion The stereochemistry has important influence on the antifungal activities of the title compounds.

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What this paper is about

Aim To study the effect of the triazole derivatives with the side chain containing(4-substituted-piperidine)-1-yl or second amine on the antifungal activity of triazole compounds.Methods Nine title compounds were synthesized and determined by the elementary analysis,()~1H-NMR and IR spectra.The MICs of all the title compounds were determined by the method recommended by the national committee for clinical laboratory standards(NCCLS)using the RPMI 1640 test medium.Results All of the title compounds displayed potent antifungal activities to some extent.The activity of the two compounds 4,5 were more than 4 times as high as that of fluconazole and itraconazole against Candida albicans in vitro.Conclusion The stereochemistry has important influence on the antifungal activities of the title compounds.

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Available abstract

Aim To study the effect of the triazole derivatives with the side chain containing(4-substituted-piperidine)-1-yl or second amine on the antifungal activity of triazole compounds.Methods Nine title compounds were synthesized and determined by the elementary analysis,()~1H-NMR and IR spectra.The MICs of all the title compounds were determined by the method recommended by the national committee for clinical laboratory standards(NCCLS)using the RPMI 1640 test medium.Results All of the title compounds displayed potent antifungal activities to some extent.The activity of the two compounds 4,5 were more than 4 times as high as that of fluconazole and itraconazole against Candida albicans in vitro.Conclusion The stereochemistry has important influence on the antifungal activities of the title compounds.

Key concepts: Chemistry, Piperazine, Fluconazole, Piperidine, Itraconazole, Antifungal, Triazole, Candida albicans

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Synthesis and antifungal activities of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted-piperazine)-1-yl]-2-propanols — Research Paper | ScholarLens