title: 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.
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Kwang-Seop
authors.initials: KS
authors.lastname: Song
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Suk Ho
authors.initials: SH
authors.lastname: Lee
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Min Ju
authors.initials: MJ
authors.lastname: Kim
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Hee Jeong
authors.initials: HJ
authors.lastname: Seo
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Junwon
authors.initials: J
authors.lastname: Lee
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Sung-Han
authors.initials: SH
authors.lastname: Lee
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Myung Eun
authors.initials: ME
authors.lastname: Jung
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Eun-Jung
authors.initials: EJ
authors.lastname: Son
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: MinWoo
authors.initials: M
authors.lastname: Lee
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Jeongmin
authors.initials: J
authors.lastname: Kim
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
authors.forename: Jinhwa
authors.initials: J
authors.lastname: Lee
keywords: SAR; SGLT2; Thiazole; diabetes; glucoside