Jiang Yuanying
2004
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Influential Citations
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Quality indicators
Journal
Chinese Journal of Medicinal Chemistry
Abstract
Aim To design and synthesize 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols and 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted sulfur ether-2-propanols and investigate their antifungal activities in vitro.Methods The desired compounds were synthesized through the reaction of the intermediate epoxide and 4-alkyloxyphenylpiperazines or substituted sulfur alcohols and confirmed by the elementary analysis,~1H-NMR and IR spectra.MIC_(80) of all the title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards(NCCLS)using the RPMI1640 test medium.Results Twelve compounds were synthesized.The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent.The antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols was more potent than that of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted sulfur ether-2-propanols in vitro.Conclusion The antifungal activities of the four compounds in 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols are more potent than that of fluconazole or equal to that of ketoconazole in vitro.