新型L-木糖衍生物作为选择性钠依赖性葡萄糖协同转运蛋白2（SGLT2）抑制剂用于治疗2型糖尿病。
Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
作者信息
Goodwin Nicole C, Mabon Ross, Harrison Bryce A, Shadoan Melanie K, Almstead Zheng Y, Xie Yiling, Healy Jason, Buhring Lindsey M, DaCosta Christopher M, Bardenhagen Jennifer, Mseeh Faika, Liu Qingyun, Nouraldeen Amr, Wilson Alan G E, Kimball S David, Powell David R, Rawlins David B
机构信息
Department of Medicinal Chemistry, Lexicon Pharmaceuticals, 350 Carter Road, Princeton, New Jersey 08540, USA.
出版信息
J Med Chem. 2009 Oct 22;52(20):6201-4. doi: 10.1021/jm900951n.
The prevalence of diabetes throughout the world continues to increase and has become a major health issue. Recently there have been several reports of inhibitors directed toward the sodium-dependent glucose cotransporter 2 (SGLT2) as a method of maintaining glucose homeostasis in diabetic patients. Herein we report the discovery of the novel O-xyloside 7c that inhibits SGLT2 in vitro and urinary glucose reabsorption in vivo.
糖尿病在全球的患病率持续上升，已成为一个主要的健康问题。最近，有几份关于针对钠依赖性葡萄糖协同转运蛋白2（SGLT2）的抑制剂的报告，作为维持糖尿病患者葡萄糖稳态的一种方法。在此，我们报告了新型O-木糖苷7c的发现，它在体外抑制SGLT2，并在体内抑制尿糖重吸收。
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