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

被引:0
作者
Eto, H
Kaneko, Y
Sakamoto, T
机构
[1] SS Pharmaceut Co Ltd, Cent Res Labs, Chiba 2868511, Japan
[2] Tohoku Univ, Grad Sch Pharmaceut Sci, Aoba Ku, Sendai, Miyagi 9808578, Japan
关键词
antifungal; 1,2,4-triazole; difluoro(heteroaryl)methyl derivatives;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New 1,2,4-triazoles (1) having a difluoro(heteroaryl)methyl moiety were designed and synthesized via 1-aryl-2,2-difluoro-2-(heteroaryl)ethanones (2), which were prepared by two routes starting from the reaction of ethyl 2,2-difluoro(heteroaryl)acetate with phenyllithiums (Route A) and from the reaction of chlorodifluoro(heteroaryl)methane with benzaldehydes (Route B), The compounds 1 except for 1g show antifungal activities against yeasts and filamentous fungi in vtiro, especially (+)-1f have equal or superior activities compared to those of itraconazole.
引用
收藏
页码:982 / 990
页数:9
相关论文
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