Abstract: Vancomycin was enlisted as a drug of the last resort for the treatment of resistant gram-positive bacterial infections. However, the emergence of vancomycin-resistant bacteria has created an urgent need for new active analogues of vancomycin. Summing up the last ten years work of this field, the review introduced the antibiotic mechanism of vancomycin and summarized the vancomycin derivatives based on the modifications of vancomycin, dimmer of vancomycin and the vancomycin mimetics. The connection of modified location and function with antibacterial activity was also discussed.