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Thiadiazole‐based Thioglycosides as Sodium‐glucose Co‐transporter 2 (SGLT2) Inhibitors
Author(s) -
Gao Yunlong,
Zhao Guilong,
Liu Wei,
Wang Yuli,
Xu Weiren,
Wang Jianwu
Publication year - 2010
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201090120
Subject(s) - chemistry , d glucose , phenylacetic acid , in vivo , sodium , combinatorial chemistry , pharmacology , organic chemistry , medicine , microbiology and biotechnology , biology
A series of thiadiazole‐based thioglycosides were synthesized as SGLT2 inhibitors from D ‐glucose, D ‐galactose and a variety of phenylacetic acids via a convenient protocol in 8 steps and evaluated in vivo with an oral glucose tolerance test (OGTT), and 5‐benzyl‐1,3,4‐thiadiazol‐2‐yl 1‐thio‐ β ‐ D ‐glucopyranoside ( 1a ) was the most efficacious to suppress the blood glucose excursion during OGTT.