Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 4, Pages 1236-1251Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm401780b
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Funding
- Shanghai Municipal Committee of Science and Technology [10431903100]
- National Basic Research Program of China (973 Program) [2010CB912603]
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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 activities against hSGLT2. In particular, deuterated compound 41 has the potential to be a robust long-acting antidiabetic agent.
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