The invention discloses a novel glycopeptide antibiotic derivative shown as in general formula (I) that is shown in the description, its pharmaceutically acceptable salts and a preparation method of the salts, wherein R1 is substituted or non-substituted benzene ring and diphenyl ring, a substituent of the substituted benzene ring and diphenyl ring is an alkoxy group, nitro group or isopropyl group with single or multiple halogens, hydroxy radicals, amino groups and C1-C9, and R2 is H. In addition, the invention also provides a pharmaceutical composition containing the glycopeptide antibiotic derivative and its pharmaceutically acceptable salts as active ingredients, and application of the pharmaceutical composition. The compound and pharmaceutical composition provided herein have good antibacterial activity and are significant to the development of novel antibacterial drugs.