Discovery of 6-Deoxydapagliflozin as a Highly Potent Sodium-dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes

Author(s): Lingyu Zhang, Yuli Wang, Huaqiang Xu, Yongheng Shi, Bingni Liu, Qunchao Wei, Weiren Xu, Lida Tang, Jianwu Wang, Guilong Zhao.

Journal Name: Medicinal Chemistry

Volume 10 , Issue 3 , 2014

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Abstract:

Systematic mono-deoxylation of the four hydroxyl groups in the glucose moiety in dapagliflozin led to the discovery of 6-deoxydapagliflozin 1 as a more active sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor (IC50 = 0.67 nM against human SGLT2 (hSGLT2) vs 1.16 nM for dapagliflozin). It exhibited more potent blood glucose inhibitory activity in rat oral glucose tolerance test and induced more urinary glucose in rat urinary glucose excretion test than its parent compound dapagliflozin.

Keywords: Dapagliflozin, deoxy, SGLT2 inhibitor, synthesis.

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Article Details

VOLUME: 10
ISSUE: 3
Year: 2014
Page: [304 - 317]
Pages: 14
DOI: 10.2174/15734064113096660051
Price: $58

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