Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 17, Pages 4770-4773Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.07.109
Keywords
diabetes; metabolism; glucosidase; metabolic diseases; NIDDM; C-glucoside; C-arylglucoside; SGLT; SGLT2; sodium-dependent glucose transporter; hyperglycemia; glucosuria; phlorizin; dapagliflozin; glucosidase
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Inhibition of sodium-dependent glucose transporter 2 (SGLT2), the transporter that is responsible for renal re-uptake of glucose, leads to glucosuria in animals. SGLT-mediated glucosuria provides a mechanism to shed excess plasma glucose to ameliorate diabetes-related hyperglycemia and associated complications. The current study demonstrates that the proper relationship of a 4'-substituted benzyl group to a beta-1C-phenylglucoside is important for potent and selective SGLT2 inhibition. The lead C-arylglucoside (7a) demonstrates superior metabolic stability to its O-arylglucoside counterpart ( 4) and it promotes glucosuria when administered in vivo. (C) 2008 Elsevier Ltd. All rights reserved.
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