Thiadiazole-based Thioglycosides as Sodium-glucose Co-transporter 2(SGLT2)Inhibitors |
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| Authors: | Gao Yunlong Zhao Guilong Liu Wei Wang Yuli Xu Weiren Wang Jianwu |
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| Institution: | 1. School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China;2. Tel.: 0086‐0531‐88362708;3. Fax: 0086‐0531‐88564464;4. Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China |
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| Abstract: | A series of thiadiazole‐based thioglycosides were synthesized as SGLT2 inhibitors from D‐glucose, D‐galactose and a variety of phenylacetic acids via a convenient protocol in 8 steps and evaluated in vivo with an oral glucose tolerance test (OGTT), and 5‐benzyl‐1,3,4‐thiadiazol‐2‐yl 1‐thio‐β‐D‐glucopyranoside ( 1a ) was the most efficacious to suppress the blood glucose excursion during OGTT. |
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| Keywords: | sodium‐glucose cotransporter 2 (SGLT2) thiadiazole synthetic methods oral glucose tolerance test (OGTT) biological activity |
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