First People's Hospital of Shangqiu, Henan Province, Shangqiu, 476000, China.
The Rogel Cancer Center, Department of Internal Medicine, University of Michigan, Ann Arbor, MI, 48109, United States.
Eur J Med Chem. 2024 Apr 5;269:116343. doi: 10.1016/j.ejmech.2024.116343. Epub 2024 Mar 18.
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.
钠-葡萄糖协同转运蛋白 2(SGLT2)抑制剂是一类小分子药物,近年来因其在 2 型糖尿病(T2DM)治疗中的潜在临床应用而受到广泛关注。这些抑制剂通过阻碍肾脏重吸收葡萄糖的能力,导致尿中葡萄糖排泄(UGE)增加,从而降低血糖水平。几种 SGLT2 抑制剂,如达格列净、卡格列净和恩格列净,已获得监管机构批准,目前可用于临床。这些抑制剂在改善血糖控制、减轻体重和降低 T2DM 患者血压方面表现出显著的效果。此外,它们在降低这组患者发生心血管事件和肾脏并发症的可能性方面也显示出潜在的优势。本文综述了小分子 SGLT2 抑制剂的合成及临床应用,为 T2DM 的治疗提供了新的治疗方法。