The invention discloses an orixine derivative and an application of orixine derivative in preparation of medicine for resisting drug-fast bacteria, the test shows that the orixine derivative is capable of inhibiting breeding of a plurality of drug-fast bacterium in vitro, and can be used for preparing antibiotic medicines for resisting drug-fast bacteria; the orixine derivative is used for preparing medicines for resisting methicillin-resistant staphylococcus aureus (MRSA), preparing medicines for resisting benzylpenicillin-resistant staphylococcus aureus, and preparing medicines for resisting vancomycin-resistant enterococcus; the medicines can be prepared to the injection, tablet, pill, capsule, a suspending agent or an emulsion for usage, a chemical structural formula of the orixine derivative is shown in formula I, wherein R1,R2 and R3 are defined in a specification.