Based on the structure of the active site of CYP51 and the structure–activity relationships of azole antifungal compounds that we designed in a previous study, a series of 1‐{1‐[2‐(substitutedbenzyloxy)ethyl]‐1H‐1,2,3‐triazol‐4‐yl}‐2‐(2,4‐difluorophenyl)‐3‐(1H‐1,2,4‐triazol‐1‐yl)propan‐2‐ols (6a–n) were designed and synthesized utilizing copper‐catalyzed azide‐alkyne cycloaddition. Preliminary antifungal tests against eight human pathogenic fungi in vitro showed that all the title compounds exhibited excellent antifungal activities with a broad spectrum in vitro. Molecular docking results indicated that the interaction between the title compounds and CYP51 comprised π–π interactions, hydrophobic interactions, and the narrow hydrophobic cleft.