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

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.

SUBMITTER: Song KS

PROVIDER: S-EPMC4018110 | biostudies-literature | 2011 Feb

REPOSITORIES: biostudies-literature

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

Song Kwang-Seop KS Lee Suk Ho SH Kim Min Ju MJ Seo Hee Jeong HJ Lee Junwon J Lee Sung-Han SH Jung Myung Eun ME Son Eun-Jung EJ Lee MinWoo M Kim Jeongmin J Lee Jinhwa J

ACS medicinal chemistry letters 20101213 2

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. ...[more]

PMID: 24900297

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