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目的钠-葡萄糖共转运蛋白2(SGLT2)是肾小管上负责将尿糖重新吸收为血糖的重要转运蛋白,对该蛋白的抑制可以使糖从血液中转移进入尿液。本文总结了目前各大药物公司在研的SGLT2抑制剂的构效关系及其临床研究进展。方法综述了近年来国内外相关报道,对O,C,N-糖苷类和非糖苷类SGLT2抑制剂的药理、药效和药代学进行讨论,并就其临床研究及开发上市状况进行概述。结果 SGLT2抑制剂的结构与其药理活性和代谢稳定性间的关系是该类药物研发的重点。结论 SGLT2抑制剂与降糖作用的构效关系,对开发新一代治疗糖尿病药物具有重要意义。
Purpose Sodium-glucose cotransporter 2 (SGLT2) is an important transporter responsible for reabsorption of urine glucose into the renal tubules, and inhibition of this protein allows sugar to be transferred from the blood into the urine. This article summarizes the current structure-activity relationship of SGLT2 inhibitors and their clinical research progress in the major drug companies. Methods This review summarizes recent reports both at home and abroad. The pharmacology, pharmacodynamics and pharmacokinetics of O, C, N-glycosides and non-glycoside SGLT2 inhibitors are reviewed. The clinical research and market status of SGLT2 inhibitors are summarized. Results The relationship between the structure of the SGLT2 inhibitor and its pharmacological activity and metabolic stability is the focus of this type of drug development. Conclusion The structure-activity relationship between SGLT2 inhibitor and hypoglycemic effect is of great significance for the development of a new generation of drugs for the treatment of diabetes.