The incidence of life-threatening fungal infections has dramatically increased for decades. In order to develop novel antifungal agents, two series of (2R,3R)-1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(N-substitutied)-2-butanols (3a-o, 5a-f, 8a-u), which were analogues of voriconazole, were designed, synthesized and characterized by ¹H NMR, ¹³C NMR and HRMS. The MIC₈₀ values showed that the target compounds 3a-o indicated better activities than fluconazole on three important fungal pathogens except for 3i. Significant activity of compounds 3d, 3k, 3n, 3m and 3o was observed on the Aspergillus fumigatus strain (MIC₈₀ range: 1–0.125 μg/ml). Especially, compound 3k had strong activity to inhibit the growth of ten fungal pathogens. But it didn't exhibit good activity in in vivo value. Molecular docking experiments demonstrated that 3k possessed superior affinity with target enzyme by strong hydrogen bond from morpholine ring.

几十年来，威胁生命的真菌感染的发生率急剧增加。为了开发新型抗真菌剂，开发了两个系列的（2 R，3 R）-1-（1 H -1,2,4-三唑-1-基）-2-（2,4-二氟苯基）-3-设计，合成了伏立康唑的类似物（N-取代）-2-丁醇（3a-o，5a-f，8a-u），并通过¹ H NMR，¹³ C NMR和HRMS进行了表征。MIC ₈₀值表明，目标化合物3a-o对除3i以外的三种重要真菌病原体的活性均优于氟康唑。。在烟曲霉菌株（MIC ₈₀范围：1-0.125μg/ ml）上观察到了化合物3d，3k，3n，3m和3o的显着活性。特别地，化合物3k具有抑制十种真菌病原体生长的强活性。但是它在体内价值上没有表现出良好的活性。分子对接实验表明3k通过吗啉环的强氢键与目标酶具有优异的亲和力。