Journal
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
Volume 30, Issue 5, Pages 785-793Publisher
HIGHER EDUCATION PRESS
DOI: 10.1007/s40242-014-4043-9
Keywords
SGLT2 inhibitor; Structure-activity relationship; Dapagliflozin
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Funding
- National Natural Science Foundation of China [21302141]
- Key Projects of Tianjin Science and Technology Support Plan, China [10ZCKFSH01300]
- Tianjin Municipal Natural Science Foundation, China [14JCQNJC12900]
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Structural modifications of 3-OH in the glucose moiety of dapagliflozin(1), an approved potent sodium-dependent glucose transporter 2(SGLT2) inhibitor, led to 3-oxodapagliflozin(16), a highly potent and more selective SGLT2 inhibitor[IC50(hSGLT1)/IC50(hSGLT2)=2851 for compound 16 vs. 843 for compound 1]. 3-Oxodapagliflozin(16) exhibited in vitro(IC50=1.0 nmol/L against hSGLT2 for compound 16 vs. 1.3 nmol/L for compound 1) and in vivo activities comparable to those of dapagliflozin(1). The bioactivities of 3-oxodapagliflozin (16) warrant its further evaluation as a promising SGLT2 inhibitor for the treatment of type 2 diabetes.
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