Discovery of non-glucoside SGLT2 inhibitors.

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

Discovery of non-glucoside SGLT2 inhibitors.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2472-5. doi: 10.1016/j.bmcl.2011.02.056. Epub 2011 Feb 24.

PubMed ID

21398124 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dapagliflozin	Sodium/glucose cotransporter 2	IC 50 (nM)	4	N/A	N/A	Details
Dapagliflozin	Sodium/glucose cotransporter 2	IC 50 (nM)	22	N/A	N/A	Details