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YAN Yong-zheng, CHAI Xiao-yun, ZOU Yan, YU Shi-chong, WU Qiu-ye. 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 358-361.
Citation:
YAN Yong-zheng, CHAI Xiao-yun, ZOU Yan, YU Shi-chong, WU Qiu-ye. 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 358-361.
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
Received Date: 2010-12-28
Rev Recd Date:
2011-05-30
Abstract
Objective To study the antifungal activity of triazole alcohols which introduce isopropyl as side chain. Methods By introduction of 4-carboxylic ester substituted benzyl group as side chain, a series of title compounds were synthesized. All of them were confirmed by MS, 1H-NMR, et al. The antifungal activities were also evaluated against eight tested pathogenic fungi. Results Fourteen title compounds were synthesized. All title compounds exhibited activity against tested fungi to some extent. Compounds (1) and (2) exhibited stronger antifungal activities against eight fungi except Aspergillus fumigatus than the control drug of itraconazole. Conclusions The introduction of 4-carboxylic ester substituted benzyl group as side chain was beneficial to improve their antifungal activity. The shorter in the side chain , the better of the antifungal activity.
Edmond MB, Wallace SE, McClish DK, et al. Nosocomial bloodstream infections in United States hospitals: a three-year analysis[J]. Clin Infect Dis, 1999, 29 (2): 234.
[2]
Nuccil M, Marr KA. Emerging fungal diseases[J]. Clin Infect Dis, 2005, 41: 521.
[3]
Zhao QJ, Song Y, Hu HG, et al. Design, synthesis and antifungal activity of novel triazole derivatives[J]. Chin Chem Lett, 2007, 18: 670.
[4]
Zhao QJ, Hu HG, Li YW, et al. Design, Synthesis, and antifungal activities of novel 1H-triazole derivatives based on the structure of the active site of fungal lanosterol 14a-demethylase (CYP51)[J]. Chem Biol, 2007, 4: 1472.
National Committee for Clinical Laboratory Standards. Reference method for broth dilution antifungal susceptibility testing of yeasts, approved standard.Document M27-A2[S].PA:Wayne: 2002.
Abstract: Objective To study the antifungal activity of triazole alcohols which introduce isopropyl as side chain. Methods By introduction of 4-carboxylic ester substituted benzyl group as side chain, a series of title compounds were synthesized. All of them were confirmed by MS, 1H-NMR, et al. The antifungal activities were also evaluated against eight tested pathogenic fungi. Results Fourteen title compounds were synthesized. All title compounds exhibited activity against tested fungi to some extent. Compounds (1) and (2) exhibited stronger antifungal activities against eight fungi except Aspergillus fumigatus than the control drug of itraconazole. Conclusions The introduction of 4-carboxylic ester substituted benzyl group as side chain was beneficial to improve their antifungal activity. The shorter in the side chain , the better of the antifungal activity.
YAN Yong-zheng, CHAI Xiao-yun, ZOU Yan, YU Shi-chong, WU Qiu-ye. 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 358-361.
Citation:
YAN Yong-zheng, CHAI Xiao-yun, ZOU Yan, YU Shi-chong, WU Qiu-ye. 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 358-361.
Edmond MB, Wallace SE, McClish DK, et al. Nosocomial bloodstream infections in United States hospitals: a three-year analysis[J]. Clin Infect Dis, 1999, 29 (2): 234.
[2]
Nuccil M, Marr KA. Emerging fungal diseases[J]. Clin Infect Dis, 2005, 41: 521.
[3]
Zhao QJ, Song Y, Hu HG, et al. Design, synthesis and antifungal activity of novel triazole derivatives[J]. Chin Chem Lett, 2007, 18: 670.
[4]
Zhao QJ, Hu HG, Li YW, et al. Design, Synthesis, and antifungal activities of novel 1H-triazole derivatives based on the structure of the active site of fungal lanosterol 14a-demethylase (CYP51)[J]. Chem Biol, 2007, 4: 1472.
National Committee for Clinical Laboratory Standards. Reference method for broth dilution antifungal susceptibility testing of yeasts, approved standard.Document M27-A2[S].PA:Wayne: 2002.
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