Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors.
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Lee SH, Kim MJ, Lee SH, Kim J, Park HJ, Lee J
Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors.
Eur J Med Chem. 2011 Jul;46(7):2662-75. doi: 10.1016/j.ejmech.2011.03.052. Epub 2011 Apr 2.
- PubMed ID
- 21514014 [ View in PubMed]
- Abstract
In order to investigate SAR regarding proximal phenyl ring in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on proximal phenyl ring was conducted. During a series of lead optimization efforts, ortho-allyloxyphenyl 10p or ortho-hydroxyphenyl 11a showed subnanomolar inhibitory activity against hSGLT2.
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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