Discovery of non-glucoside SGLT2 inhibitors

AR Li, J Zhang, J Greenberg, TW Lee, J Liu

Index: Li, An-Rong; Zhang, Jian; Greenberg, Joanne; Lee, Taeweon; Liu, Jiwen Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2472 - 2475

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Citation Number: 24

Abstract

A series of benzothiazinone and benzooxazinone derivatives were discovered as SGLT2 inhibitors. The optimization led to the discovery of compounds 31 and 32, which exhibited similar potency and better SGLT1 selectivity compared to dapagliflozin. These compounds may provide novel promising scaffolds, which are different from phlorizin-based SGLT2 inhibitors.