2. Academic Validation
  3. Synthesis and SAR of Thiazolylmethylphenyl Glucoside as Novel C-Aryl Glucoside SGLT2 Inhibitors

Synthesis and SAR of Thiazolylmethylphenyl Glucoside as Novel C-Aryl Glucoside SGLT2 Inhibitors

  • ACS Med Chem Lett. 2010 Dec 13;2(2):182-7. doi: 10.1021/ml100256c.
Kwang-Seop Song 1,  Suk Ho Lee 1,  Min Ju Kim 1,  Hee Jeong Seo 1,  Junwon Lee 1,  Sung-Han Lee 1,  Myung Eun Jung 1,  Eun-Jung Son 1,  MinWoo Lee 1,  Jeongmin Kim 1,  Jinhwa Lee 1
Affiliations

Affiliation

  • 1 Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
PMID: 24900297 DOI: 10.1021/ml100256c
Abstract

Novel C-aryl glucoside SGLT2 inhibitors containing the thiazole motif were designed and synthesized for biological evaluation. Among the compounds assayed, thiazole containing furanyl moiety 14v and thiophenyl moiety 14y demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date (IC50 = 0.720 nM for 14v and IC50 = 0.772 nM for 14y). Both of these compounds have been further evaluated on a urinary glucose excretion test and the urine volumes excreted.

Keywords

SAR; SGLT2; Thiazole; diabetes; glucoside.

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