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

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