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Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2017 Jan 26; Vol. 60 (2), pp. 710-721. Date of Electronic Publication: 2017 Jan 17. - Publication Year :
- 2017
-
Abstract
- 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.
- Subjects :
- Animals
Benzhydryl Compounds administration & dosage
Benzhydryl Compounds chemical synthesis
Benzhydryl Compounds chemistry
Glucose metabolism
Glucose Tolerance Test
Humans
Hypoglycemic Agents administration & dosage
Hypoglycemic Agents chemical synthesis
Hypoglycemic Agents chemistry
Intestinal Absorption drug effects
Male
Mice, Knockout
Phenylbutyrates administration & dosage
Phenylbutyrates chemical synthesis
Phenylbutyrates chemistry
Structure-Activity Relationship
Thioglycosides administration & dosage
Thioglycosides chemical synthesis
Thioglycosides chemistry
Benzhydryl Compounds pharmacology
Hypoglycemic Agents pharmacology
Phenylbutyrates pharmacology
Sodium-Glucose Transporter 1 antagonists & inhibitors
Thioglycosides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 60
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 28045524
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.6b01541