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SGLT2 inhibitors were promising and novel antidiabetic drugs which suppressed glucose reabsorption and increased urinary glucose exertion. This review paper are aimed to summarize the recent progress of SGLT2 inhibitors during the last 5 years. This paper first summarizes the information of SGLT2 inhibitors, including mechanism, evolution and then focuses on the recent efforts on structure-activity relationships and structural optimization of SGLT2 inhibitors. Finally, the corresponding clinical therapeutic efficacy and adverse drug reaction in patients with Type 2 diabetes are discussed in detail.