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Design, Syntheses, and SAR Studies of Carbocyclic Analogues of Sergliflozin as Potent Sodium‐Dependent Glucose Cotransporter 2 Inhibitors
Author(s) -
Shing Tony K. M.,
Ng WaiLung,
Chan Judy Y.W.,
Lau Clara B.S.
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201302543
Subject(s) - cotransporter , chemistry , transporter , renal glucose reabsorption , dapagliflozin , small molecule , combinatorial chemistry , sodium , computational biology , biochemistry , diabetes mellitus , type 2 diabetes , medicine , gene , biology , organic chemistry , endocrinology
Combating diabetes: A small‐molecule carbohydrate mimic, pseudo‐sergliflozin, was synthesized effectively by a regio‐ and stereoselective allylic substitution reaction. It was found to be a potent and selective inhibitor of a transporter protein—sodium‐dependent glucose cotransporter 2 (SGLT2)—which is responsible for glucose reabsorption in the human body. It could be a lead compound for further development into an antidiabetic agent.