Discovery of non-glucoside SGLT2 inhibitors.

Bioorg Med Chem Lett

Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.

Published: April 2011

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.

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http://dx.doi.org/10.1016/j.bmcl.2011.02.056DOI Listing

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