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

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journal contribution
posted on 10.02.2011, 00:00 authored by Kwang-Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Junwon Lee, Sung-Han Lee, Myung Eun Jung, Eun-Jung Son, MinWoo Lee, Jeongmin Kim, Jinhwa Lee
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.