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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1-[(1 H -indol-3-ylmethyl)methylamino]-3-(1 H -1,2,4-triazol-1-yl)propan-2-ols
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Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1-[(1 H -indol-3-ylmethyl)methylamino]-3-(1 H -1,2,4-triazol-1-yl)propan-2-ols

机译:2-(2,4-二氟苯基)-1-[((1 H-吲哚-3-基甲基)甲基氨基] -3-(1 H -1,2,4-三唑-1-基)的合成及体外抗真菌评价丙-2-醇

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摘要

We extended our previous studies based on the design of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents toward the identification of new indol-3-ylmethylamino derivatives. The majority of these compounds exhibited antifungal activity against a Candida albicans strain (minimum inhibitory concentrations ranging from 199.0 to 381.0?ng/mL) suggesting an inhibition of 14α-demethylase by sterol analysis studies, but are weaker inhibitors compared to their indol-5-ylmethylamino analogs.
机译:我们基于1-[((1H-吲哚-5-基甲基)氨基] -2-苯基-3-(1H-1,2,4-三唑-1-基)丙-2-的设计扩展了以前的研究醇作为抗真菌剂,用于鉴定新的吲哚-3-基甲基氨基衍生物。这些化合物中的大多数对白色念珠菌菌株均表现出抗真菌活性(最低抑菌浓度范围为199.0至381.0?ng / mL),表明通过固醇分析研究可抑制14α-脱甲基酶,但与吲哚-5-相比,它们的抑制作用较弱ylmethylamino类似物。

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