Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes

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• 作者：Nicole C. GoodwinZhi-Ming Ding ; Bryce A. Harrison ; Eric D. Strobel ; Angela L. Harris ; Melinda Smith ; Andrea Y. Thompson ; Wendy Xiong ; Faika Mseeh ; Debra J. Bruce ; Damaris Diaz ; Suma Gopinathan ; Ling Li ; Emily O’Neill ; Mary Thiel ; Alan G. E. Wilson ; Kenneth G. Carson ; David R. Powell ; David B. Rawlins
• 刊名：Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：January 26, 2017
• 年：2017
• 卷：60
• 期：2
• 页码：710-721
• 全文大小：620K
• ISSN：1520-4804

文摘

The increasing number of people afflicted with diabetes throughout the world is a major health issue. Inhibitors of the sodium-dependent glucose cotransporters (SGLT) have appeared as viable therapeutics to control blood glucose levels in diabetic patents. Herein we report the discovery of LX2761, a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.