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Volume 27 Issue 5
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2009  >  27(5): 324-327,392

WEI Ning, ZHANG Song-wei, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, WU Qiu-ye. 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[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(5): 324-327,392.
Citation: WEI Ning, ZHANG Song-wei, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, WU Qiu-ye. 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[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(5): 324-327,392.
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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

  • 1.

    Airforce General Hospital of People's Liberation Army, Beijing 100036 China

  • 2.

    Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • Received Date: 2009-06-02
  • 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,etal.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.
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    沈阳化工大学材料科学与工程学院 沈阳 110142

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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

  • 1. Airforce General Hospital of People's Liberation Army, Beijing 100036 China
  • 2. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • Received Date: 2009-06-02

Abstract: 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,etal.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.

WEI Ning, ZHANG Song-wei, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, WU Qiu-ye. 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[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(5): 324-327,392.
Citation: WEI Ning, ZHANG Song-wei, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, WU Qiu-ye. 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[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(5): 324-327,392.
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