Design, Syntheses, and SAR Studies of Carbocyclic Analogues of Sergliflozin as Potent Sodium‐Dependent Glucose Cotransporter 2 Inhibitors | Zendy

Shing Tony K. M. | Zendy; Ng WaiLung | Zendy; Chan Judy Y.W. | Zendy; Lau Clara B.S. | Zendy

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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.

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