Novel thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.
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Lee SH, Song KS, Kim JY, Kang M, Lee JS, Cho SH, Park HJ, Kim J, Lee J
Novel thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.
Bioorg Med Chem. 2011 Oct 1;19(19):5813-32. doi: 10.1016/j.bmc.2011.08.014. Epub 2011 Aug 22.
- PubMed ID
- 21906953 [ View in PubMed]
- Abstract
Novel thiophene C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different types of thiophene derivatives were readily prepared. Among the compounds tested, ethylphenyl at the distal ring 71p showed the best in vitro inhibitory activity in this series to date (IC(50)=4.47 nM) against SGLT2.
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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