1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols

YAN Yong-zheng; CHAI Xiao-yun; ZOU Yan; YU Shi-chong; WU Qiu-ye

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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.

1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols

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

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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.

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[1]	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.
[5]	吴秋业,杨济秋. 4-{[2-(1H-咪唑基)-1-(4-取代苯基)乙氧基]甲基}苯甲酸类化合物的合成及其抑制血小板聚集的作用[J]. 药学学报,1991, 26(10): 741.
[6]	孙青龑, 刘超美, 赵红兵, 等. 1-(1H-1, 2, 4-三唑-1-基)-2-(2, 4-二氟苯基)-3-含硫侧链-2-丙醇类化合物的合成及抗真菌活性[J]. 第二军医大学学报, 2001, 22(9): 871.
[7]	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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1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoroph-enyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols

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通讯作者: 陈斌, [email protected]

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