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O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors |
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| Authors: | Baihua Xu Binhua Lv Yan Feng Ge Xu Jiyan Du Ajith Welihinda Zelin Sheng Brian Seed Yuanwei Chen |
| Affiliation: | 1. Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, Sichuan 610041, PR China;2. Egret Pharma (Shanghai) Limited, Shanghai 201203, PR China;3. Graduate School of Chinese Academy of Sciences, Beijing 100049, PR China;4. Theracos, Inc., Sunnyvale, CA 94085, USA |
| Abstract: | Two series of O-spiro C-aryl glucosides were synthesized and tested for inhibition of hSGLT1 and hSGLT2. 6′-O-Spiro C-aryl glucosides exhibited potent in vitro hSGLT2 inhibitory activity but 2′-O-spiro C-aryl glucosides showed no in vitro hSGLT2 inhibitory activity at a screening concentration of 1 μM. |
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