With the development of glycomics, more and more carbohydrate mimetics were used to investigate the interactions between carbohydrate-proteins, especially in physiological and pathological processes, molecular recognition, signal transduction, cell communication, cell differentiation and developmental events. Recently, because of the drug-resistance of microorganisms and the development of antibiotics, the interactions between carbohydrate mimetics and RNAs are becoming hot issue. Aminoglycosides, one family of important antibiotics, can bind with 30S subunits of rRNA to prevent the normal translations of proteins, inhibit the proteins involving in the drug-resistance. In this review, the latest advances in development and applications of aminoglycosides are summarized and the detailed descriptions on the SAR study (Structure-activity relationship) of aminoglycoside derivatives are discussed.