Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors.

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Du X, Lizarzaburu M, Turcotte S, Lee T, Greenberg J, Shan B, Fan P, Ling Y, Medina JC, Houze J

Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3774-9. doi: 10.1016/j.bmcl.2011.04.053. Epub 2011 Apr 20.

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21565497 [ View in PubMed

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Abstract

Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharmacokinetic properties of this series of SGLT2 inhibitors. From these efforts, compounds 28 and 32 have improved solubility and pharmacokinetic properties compared to compound 1.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dapagliflozin	Sodium/glucose cotransporter 2	IC 50 (nM)	3	N/A	N/A	Details