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Bioorg Med Chem. 2011 Sep 15;19(18):5468-79. doi: 10.1016/j.bmc.2011.07.045. Epub 2011 Jul 28.

Novel macrocyclic C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.

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  • 1Research Center, Green Cross Corporation, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.


Novel macrocyclic C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different synthetic routes of macrocyclization were adopted to prepare novel ansa SGLT2 inhibitors. Among the compounds tested, [1,7]dioxacyclopentadecine macrocycles possessing methylthiophenyl at the distal ring 40 or ethoxyphenyl at the distal ring 23 showed the best in vitro inhibitory activity in this series to date (40, IC(50)=0.778 nM and 23, IC(50)=0.899 nM) against hSGLT2.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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