C-芳基糖苷类SGLT2抑制剂的发现及构效关系研究进展
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摘要
目的综述C-芳基糖苷类钠-葡萄糖协同转运蛋白2(sodium-glucose co-transporter 2,SGLT2)抑制剂的发现历程及构效关系研究.方法通过查找文献,对C-芳基糖苷类SGLT2抑制剂的发现、结构修饰及发展历程进行综述.结果目前已上市的C-芳基糖苷类SGLT2抑制剂共有6种,SGLT2抑制剂选择性抑制SGLT2,抑制肾小管对葡萄糖的重吸收作用,可在不增加体重和避免低血糖风险的情况下,改善糖尿病患者的状况,起到降糖效果.结论 C-芳基糖苷类SGLT2抑制剂研究广泛,为糖尿病的治疗提供了一种新途径.
Objective To review the discovery process and structure-activity relationship of C-aryl glycoside sodium-glucose co-transporter 2(SGLT2) inhibitors.Methods The search,structure modification and development of C-aryl glycoside SGLT2 inhibitors were reviewed by searching literature.Results There are 6 kinds of C-aryl glycoside SGLT2 inhibitors that have been marketed.SGLT2 inhibitors have selective inhibition of SGLT2.The principle behind SGLT2 inhibition involves the amelioration of diabetic conditions without increasing body weight and the risk of hypoglycemia.Improving the condition of patients with diabetes and playing a hypoglycemic effect.Conclusion C-aryl glycoside SGLT2 inhibitors are widely studied and provide a new approach for the treatment of diabetes.
Objective To review the discovery process and structure-activity relationship of C-aryl glycoside sodium-glucose co-transporter 2(SGLT2) inhibitors.Methods The search,structure modification and development of C-aryl glycoside SGLT2 inhibitors were reviewed by searching literature.Results There are 6 kinds of C-aryl glycoside SGLT2 inhibitors that have been marketed.SGLT2 inhibitors have selective inhibition of SGLT2.The principle behind SGLT2 inhibition involves the amelioration of diabetic conditions without increasing body weight and the risk of hypoglycemia.Improving the condition of patients with diabetes and playing a hypoglycemic effect.Conclusion C-aryl glycoside SGLT2 inhibitors are widely studied and provide a new approach for the treatment of diabetes.
引文
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[36] Washburn W N.Development of the renal glucose reabsorption inhibitors:a new mechanism for the pharmacotherapy of diabetes mellitus type 2[J].J.Med.Chem,2009,52(7):1785-1794.
[37] Ohtake Y,Sato T,Matsuoka H,et al.C-aryl 5a-carba-β-D-glucopyranosides as novel sodium glucose cotransporter 2(SGLT2) inhibitors for the treatment of type 2 diabetes[J].Bio Org Med Chem,2012,20(13):4117-4127.
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