Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes
详细信息 查看全文
- 作者：Wei Meng ; Bruce A. Ellsworth ; Alexandra A. Nirschl ; Peggy J. McCann ; Manorama Patel ; Ravindar N. Girotra ; Gang Wu ; Philip M. Sher ; Eamonn P. Morrison ; Scott A. Biller ; Robert Zahler ; Prashant P. Deshp
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：March 13, 2008
- 年：2008
- 卷：51
- 期：5
- 页码：1145 - 1149
- 全文大小：202K
- 年卷期：v.51,no.5(March 13, 2008)
- ISSN：1520-4804
文摘
The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats. These findings, combined with a favorable ADME profile, have prompted clinical evaluation of dapagliflozin for the treatment of type 2 diabetes.