New antifungal 1,2,4-triazoles with difluoro(substituted sulfonyl)methyl moiety

被引:63
作者
Eto, H [1 ]
Kaneko, Y [1 ]
Takeda, S [1 ]
Tokizawa, M [1 ]
Sato, S [1 ]
Yoshida, K [1 ]
Namiki, S [1 ]
Ogawa, M [1 ]
Maebashi, K [1 ]
Ishida, K [1 ]
Matsumoto, M [1 ]
Asaoka, T [1 ]
机构
[1] SS Pharmaceut Co Ltd, Cent Res Labs, Chiba 2868511, Japan
关键词
antifungal; 1,2,4-triazole; difluoro(substituted sulfonyl)methyl derivative;
D O I
10.1248/cpb.49.173
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New 1,2,4-triazoles (2) having a difluoro(substituted sulfonyl)methyl moiety were designed and synthesized via alpha,alpha -difluoro-alpha-(substituted thio)acetophenones (3). Compounds (2) showed potent antifungal activities against C. albicans, C. krusei, A. flavus and A. fumigatus in vitro and against C. albicans in vivo for oral and i.v. administrations. Especially, (-)-2a, (-)-2b and (-)-2d showed potent antifungal activities.
引用
收藏
页码:173 / 182
页数:10
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