Design, Syntheses and SAR Studies of Carbocyclic Analogues of Sergliflozin as Potent Sodium-dependent Glucose Co-transporter 2 Inhibitors

June 19, 2013

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.


Angew. Chem. Int. Ed., 2013, 52, 8401−8405.


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