351. Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors.
- Author
-
Lee SH, Kim MJ, Lee SH, Kim J, Park HJ, and Lee J
- Subjects
- Animals, Biological Transport drug effects, CHO Cells, Carbon Radioisotopes, Cricetulus, Gene Expression, Glucosides pharmacology, Humans, Hypoglycemic Agents pharmacology, Methylglucosides metabolism, Recombinant Proteins chemistry, Small Molecule Libraries pharmacology, Sodium-Glucose Transporter 2 chemistry, Structure-Activity Relationship, Thiazoles pharmacology, Glucosides chemical synthesis, Hypoglycemic Agents chemical synthesis, Small Molecule Libraries chemical synthesis, Sodium-Glucose Transporter 2 Inhibitors, Thiazoles chemical synthesis
- 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., (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
- Published
- 2011
- Full Text
- View/download PDF