目前，钠–葡萄糖协同转运蛋白2（SGLT2）抑制剂通过抑制葡萄糖在肾脏近曲小管的重吸收，从而成为治疗糖尿病的新途径。按其结构，SGLT2抑制剂主要分为C-芳基抑制剂、O-芳基抑制剂、S-糖苷抑制剂和N-糖苷抑制剂，而C-芳基抑制剂和O-芳基抑制剂处于研究热点，其中几个新药（dapagliflozin、canagliflozin、ASP1941、BI10773和LX4211）显示出良好的控制血糖水平和减轻体质量的效果，且不良反应较小。综述两类结构中的主要药物研究概况，并分析其研发前景。

For the present, sodium-glucose co-transporter 2 (SGLT2) inhibitors have become a potentially new therapeutic approach for the treatment of type 2 diabetes, and they could lower the blood glucose levels by inhibiting glucose reabsorption in the renal proximal tubules. They conclude C-aryl inhibitor, O-aryl inhibitor, S-aryl inhibitor, and N-aryl inhibitor, but C-aryl inhibitor and O-aryl inhibitor are in the hot research. Several SGLT2 inhibitors in development (dapagliflozin, canagliflozin, ASP1941, BI10773, and LX4211) have demonstrated the improvement in glycemic control and weight loss, along with slight adverse effects. In this paper, the progress in study on drugs, from the two sorts of structure, is reviewed, and the development prospects of the SGLT2 is also analyzed.

国家重大新药创制专项（2011ZX09401-009），天津市科技支撑计划重点项目（10ZCKFSH01300）