Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors.

Article Details

Citation

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DapagliflozinSodium/glucose cotransporter 2IC 50 (nM)0.49N/AN/ADetails