2. Academic Validation
  3. Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2

Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2

  • Bioorg Med Chem Lett. 2011 Jan 15;21(2):742-6. doi: 10.1016/j.bmcl.2010.11.115.
Eun-Jung Park 1,  Younggyu Kong,  Jun Sung Lee,  Sung-Han Lee,  Jinhwa Lee
Affiliations

Affiliation

  • 1 Green Cross Corporation, Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
PMID: 21193308 DOI: 10.1016/j.bmcl.2010.11.115
Abstract

In order to investigate SAR regarding glucose moiety in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on glucose was conducted to explore potential utility as a suitable replacement of glucose per se. Among the compounds prepared, deshydroxy 29 (IC(50)=7.01nM) demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date. But, none of the compounds were better than the parent molecule 5 (IC(50)=1.75nM).

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