目前，鈉–葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋白2（SGLT2）抑制劑通過抑制葡萄糖在腎臟近曲小管的重吸收，從而成為治療糖尿病的新途徑。按其結(jié)構(gòu)，SGLT2抑制劑主要分為C-芳基抑制劑、O-芳基抑制劑、S-糖苷抑制劑和N-糖苷抑制劑，而C-芳基抑制劑和O-芳基抑制劑處于研究熱點(diǎn)，其中幾個(gè)新藥（dapagliflozin、canagliflozin、ASP1941、BI10773和LX4211）顯示出良好的控制血糖水平和減輕體質(zhì)量的效果，且不良反應(yīng)較小。綜述兩類結(jié)構(gòu)中的主要藥物研究概況，并分析其研發(fā)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.

國(guó)家重大新藥創(chuàng)制專項(xiàng)（2011ZX09401-009），天津市科技支撐計(jì)劃重點(diǎn)項(xiàng)目（10ZCKFSH01300）