Discovery of dapagliflozin: A potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes

被引：536

作者：

Meng, Wei ^{[1
]}

Ellsworth, Bruce A. ^{[1
]}

Nirschl, Alexandra A. ^{[1
]}

McCann, Peggy J. ^{[1
]}

Patel, Manorama ^{[1
]}

Girotra, Ravindar N. ^{[1
]}

Wu, Gang ^{[1
]}

Sher, Philip M. ^{[1
]}

Morrison, Eamonn P. ^{[1
]}

Biller, Scott A. ^{[1
]}

Zahler, Robert ^{[1
]}

Deshpande, Prashant P. ^{[2
]}

Pullockaran, Annie ^{[2
]}

Hagan, Deborah L. ^{[3
]}

Morgan, Nathan ^{[3
]}

Taylor, Joseph R. ^{[3
]}

Obermeier, Mary T. ^{[4
]}

Humphreys, William G. ^{[4
]}

Khanna, Ashish ^{[4
]}

Discenza, Lorell ^{[4
]}

Robertson, James G. ^{[3
]}

Wang, Aiying ^{[3
]}

Hang, Songping ^{[3
]}

Wetterau, John R.

Janovitz, Evan B. ^{[5
]}

Flint, Oliver P. ^{[5
]}

Whaley, Jean M. ^{[3
]}

Washburn, William N. ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Metab Dis Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Proc R&D, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Co, Metab Dis Biol, Princeton, NJ 08543 USA

[4] Bristol Myers Squibb Co, Pharmacol Candidate Optimizat, Princeton, NJ 08543 USA

[5] Bristol Myers Squibb Co, Drug Safety Evaluat, Princeton, NJ 08543 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 05期

关键词：

D O I：

10.1021/jm701272q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1145 / 1149

页数：5

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