1. Synthesis and biological evaluation of novel C-aryl d-glucofuranosides as sodium-dependent glucose co-transporter 2 inhibitors.
- Author
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Lin TS, Liw YW, Song JS, Hsieh TC, Yeh HW, Hsu LC, Lin CJ, Wu SH, and Liang PH
- Subjects
- Animals, Benzhydryl Compounds chemistry, Benzhydryl Compounds metabolism, CHO Cells, Cricetinae, Cricetulus, Glucosidases chemistry, Glucosidases metabolism, Glucosides chemical synthesis, Glucosides metabolism, Humans, Phlorhizin chemistry, Protein Binding, Sodium-Glucose Transporter 1 antagonists & inhibitors, Sodium-Glucose Transporter 1 genetics, Sodium-Glucose Transporter 1 metabolism, Sodium-Glucose Transporter 2 genetics, Sodium-Glucose Transporter 2 metabolism, Structure-Activity Relationship, Benzhydryl Compounds chemical synthesis, Glucosidases chemical synthesis, Glucosides chemistry, Sodium-Glucose Transporter 2 Inhibitors
- Abstract
Novel C-aryl-d-glucofuranosides were synthesized and evaluated for their capacity to inhibit human sodium-dependent glucose co-transporter 2 (hSGLT2) and hSGLT1. Compound 21q demonstrated the best in vitro inhibitory activity against SGLT2 in this series (EC50=0.62μM)., (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Published
- 2013
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