Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2.
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Park EJ, Kong Y, Lee JS, Lee SH, Lee J
Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2.
Bioorg Med Chem Lett. 2011 Jan 15;21(2):742-6. doi: 10.1016/j.bmcl.2010.11.115. Epub 2010 Dec 3.
- PubMed ID
- 21193308 [ View in PubMed]
- Abstract
In order to investigate SAR regarding glucose moiety in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on glucose was conducted to explore potential utility as a suitable replacement of glucose per se. Among the compounds prepared, deshydroxy 29 (IC(50)=7.01nM) demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date. But, none of the compounds were better than the parent molecule 5 (IC(50)=1.75nM).
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Dapagliflozin Sodium/glucose cotransporter 2 IC 50 (nM) 0.49 N/A N/A Details