Design, Synthesis, and Biological Evaluation of Deuterated C‑Aryl Glycoside as a Potent and Long-Acting Renal Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes

SGLT2 inhibitors deuterated at sites susceptible to oxidative metabolism were found to have a slightly longer t max and half-life (t 1/2), dose-dependent increase in urinary glucose excretion (UGE) in rats, and slightly superior effects on UGE in dogs while retaining similar in vitro inhibitory acti...

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Veröffentlicht in:	Journal of medicinal chemistry 2014-02, Vol.57 (4), p.1236-1251
Hauptverfasser:	Xu, Ge, Lv, Binhua, Roberge, Jacques Y, Xu, Baihua, Du, Jiyan, Dong, Jiajia, Chen, Yuanwei, Peng, Kun, Zhang, Lili, Tang, Xinxing, Feng, Yan, Xu, Min, Fu, Wei, Zhang, Wenbin, Zhu, Liangcheng, Deng, Zhongping, Sheng, Zelin, Welihinda, Ajith, Sun, Xun
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Diabetes Mellitus, Type 2 - drug therapy Glycosides - chemical synthesis Glycosides - chemistry Glycosides - pharmacology Magnetic Resonance Spectroscopy Rats Rats, Sprague-Dawley Sodium-Glucose Transporter 2 - antagonists & inhibitors Spectrometry, Mass, Electrospray Ionization
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