2. Academic Validation
  3. Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors

Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors

  • Eur J Med Chem. 2011 Jul;46(7):2662-75. doi: 10.1016/j.ejmech.2011.03.052.
Suk Ho Lee 1,  Min Ju Kim,  Sung-Han Lee,  Jeongmin Kim,  Hyun-Ju Park,  Jinhwa Lee
Affiliations

Affiliation

  • 1 Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
PMID: 21514014 DOI: 10.1016/j.ejmech.2011.03.052
Abstract

In order to investigate SAR regarding proximal phenyl ring in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on proximal phenyl ring was conducted. During a series of lead optimization efforts, ortho-allyloxyphenyl 10p or ortho-hydroxyphenyl 11a showed subnanomolar inhibitory activity against hSGLT2.

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