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Synthetic approaches and clinical application of small-molecule inhibitors of sodium-dependent glucose transporters 2 for the treatment of type 2 diabetes mellitus
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2024-03-18 , DOI: 10.1016/j.ejmech.2024.116343
Tong Xie , Li-Jie Zhao

Sodium-dependent glucose transporters 2 (SGLT2) inhibitors are a class of small-molecule drugs that have gained significant attention in recent years for their potential clinical applications in the treatment of type 2 diabetes mellitus (T2DM). These inhibitors function by obstructing the kidneys' ability to reabsorb glucose, resulting in a rise in the excretion of glucose in urine (UGE) and subsequently lowering blood glucose levels. Several SGLT2 inhibitors, such as Dapagliflozin, Canagliflozin, and Empagliflozin, have been approved by regulatory authorities and are currently available for clinical use. These inhibitors have shown notable enhancements in managing blood sugar levels, reducing body weight, and lowering blood pressure in individuals with T2DM. Additionally, they have exhibited potential advantages in decreasing the likelihood of cardiovascular incidents and renal complications among this group of patients. This review article focuses on the synthesis and clinical application of small-molecule SGLT2 inhibitors, which have provided a new therapeutic approach for the management of T2DM.

中文翻译:

钠依赖性葡萄糖转运蛋白2小分子抑制剂治疗2型糖尿病的合成方法及临床应用

钠依赖性葡萄糖转运蛋白2(SGLT2)抑制剂是一类小分子药物,近年来因其在治疗2型糖尿病(T2DM)方面的潜在临床应用而受到广泛关注。这些抑制剂的作用是阻碍肾脏重吸收葡萄糖的能力,导致尿液中葡萄糖的排泄量 (UGE) 增加,从而降低血糖水平。达格列净、卡格列净、恩格列净等多种SGLT2抑制剂已获得监管机构批准,目前可用于临床。这些抑制剂在控制 T2DM 患者的血糖水平、减轻体重和降低血压方面显示出显着的增强作用。此外,它们在降低此类患者心血管事件和肾脏并发症的可能性方面表现出了潜在的优势。本文重点介绍小分子SGLT2抑制剂的合成及临床应用,为T2DM的治疗提供了新的治疗途径。
更新日期:2024-03-18
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