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

Autor:	Suma Gopinathan, Kenneth G. Carson, Alan G. E. Wilson, Zhi-Ming Ding, Bryce Alden Harrison, Damaris S. Diaz, Angela L. Harris, Debra Bruce, Nicole Cathleen Goodwin, Emily O’Neill, David R. Powell, Melinda Smith, Eric Strobel, David B. Rawlins, Wendy Xiong, Ling Li, Andrea Y. Thompson, Mary Thiel, Faika Mseeh
Rok vydání:	2017
Předmět:	Male 0301 basic medicine medicine.medical_specialty 030209 endocrinology & metabolism Glucose absorption Structure-Activity Relationship 03 medical and health sciences Sodium-Glucose Transporter 1 0302 clinical medicine In vivo Diabetes mellitus Internal medicine Drug Discovery medicine Animals Humans Hypoglycemic Agents Benzhydryl Compounds Glycemic Mice Knockout Chemistry Glucose Tolerance Test medicine.disease Phenylbutyrates In vitro Glucose 030104 developmental biology Endocrinology Intestinal Absorption Thioglycosides Molecular Medicine Cotransporter Sodium dependent
Zdroj:	Journal of Medicinal Chemistry. 60:710-721
ISSN:	1520-4804 0022-2623
DOI:	10.1021/acs.jmedchem.6b01541
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8541b1a58e42776d5a5b4773e40351f7 https://doi.org/10.1021/acs.jmedchem.6b01541 Zobrazit plný text záznamu