2. Academic Validation
  3. Novel macrocyclic C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents

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

  • Bioorg Med Chem. 2011 Sep 15;19(18):5468-79. doi: 10.1016/j.bmc.2011.07.045.
Min Ju Kim 1,  Suk Ho Lee,  So Ok Park,  Hyunku Kang,  Jun Sung Lee,  Ki Nam Lee,  Myung Eun Jung,  Jeongmin Kim,  Jinhwa Lee
Affiliations

Affiliation

  • 1 Research Center, Green Cross Corporation, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
PMID: 21868239 DOI: 10.1016/j.bmc.2011.07.045
Abstract

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.

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