The invention discloses derivatives of naftifine hydrochloride as well as a preparation method and application thereof. The derivatives of naftifine hydrochloride are as shown in the formula I. By inhibiting expression and/or function of key catalyzing enzyme CrtN in a golden yellow pigment synthesis pathway and powerfully inhibiting synthesis of golden yellow pigment, virulence of bacteria can be lowered. The key catalyzing enzyme CrtN in the golden yellow pigment synthesis pathway can be taken as a drug acting target; and compounds capable of inhibiting expression and/or function of key catalyzing enzyme CrtN can be used for preparing anti-bacterial drug. The naftifine hydrochloride and the derivatives thereof can be used as inhibitors for catalyzing enzyme CrtN to powerfully inhibit synthesis of the golden yellow pigment, so that the virulence of staphylococcus aureus can be lowered, and therefore, the derivatives can be used for preparing the anti-bacterial drug, especially drug for resisting staphylococcus aureus infection.