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Volume 27 Issue 2
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2009  >  27(2): 107-110

ZHANG Jie-bing, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, GU Zhuo-liang, ZHOU Guo-hua. Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(2): 107-110.
Citation: ZHANG Jie-bing, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, GU Zhuo-liang, ZHOU Guo-hua. Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(2): 107-110.
shu

Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols

  • 1.

    Institute of Drug and Instrument, Nanjing Military Area, Nanjing 210002, China

  • 2.

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

  • Received Date: 2009-02-20
  • Objective : Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole. Methods : A 4-carboxylic ester substituted benzyl group introduced and a series title compounds synthesized.All of them were confirmed by MS,1H-NMR,etal.The antifungal activities were also evaluated against the eight tested pathogenic fungi. Results :Fifteen title compounds were synthesized.All title compounds exhibited activity against fungi tested to some extent.Compounds(1),(2)and(3)exhibited strong antifungal activities against eight fungi comparable to the control drug itraconazole except Aspergillus fumigatus. Conclusions :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-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols

  • 1. Institute of Drug and Instrument, Nanjing Military Area, Nanjing 210002, China
  • 2. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • Received Date: 2009-02-20

Abstract: Objective : Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole. Methods : A 4-carboxylic ester substituted benzyl group introduced and a series title compounds synthesized.All of them were confirmed by MS,1H-NMR,etal.The antifungal activities were also evaluated against the eight tested pathogenic fungi. Results :Fifteen title compounds were synthesized.All title compounds exhibited activity against fungi tested to some extent.Compounds(1),(2)and(3)exhibited strong antifungal activities against eight fungi comparable to the control drug itraconazole except Aspergillus fumigatus. Conclusions :A benzyl moiety with a group of shorter length substituted on 4-position is required for high activity.

ZHANG Jie-bing, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, GU Zhuo-liang, ZHOU Guo-hua. Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(2): 107-110.
Citation: ZHANG Jie-bing, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, GU Zhuo-liang, ZHOU Guo-hua. Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(2): 107-110.
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