The invention discloses an isavuconazole derivative as shown in formula I shown in the description or a three-dimensional isomer thereof, wherein R1 is R2, -C(O)R2 or SO2R2; R2 is C1 to C8 alkyl substituted by 1 to 3 independent R3, -O-C1 to C8 alkyl, -C1 to C8 alkyl-CO2R4, -C1 to C8 alkyl-SO2R4, or -C1 to C8 alkyl-PO3(OH)R4; R3 is hydrogen, halogen, nitro group, amino group, cyanogroup, alkyl, alkoxy or alkynyl; R4 is hydrogen, lithium, sodium, potassium or organic amine. The invention also provides application of the compound of the formula I in preparing a fungal infection resistant drug, and the compound is good in solubility and significant in antifungal effect.