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ID: ALA1157636

Journal: Bioorg Med Chem

Title: Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners.

Authors: Lee J, Lee SH, Seo HJ, Son EJ, Lee SH, Jung ME, Lee M, Han HK, Kim J, Kang J, Lee J.

Abstract: Novel C-aryl glucoside SGLT2 inhibitors containing 1,3,4-thiadiazole moieties were designed and synthesized. Among the compounds tested, biaryl-type compounds containing pyrazine 59, 2-furan 61, and 3-thiophene 71 showed the best in vitro inhibitory activities to date (IC(50) = 3.51-7.03 nM) against SGLT2. A selected compound 61, demonstrated reasonable blood glucose-lowering effects, indicating that the information obtained from the SAR studies in this 1,3,4-thiadiazolylmethylphenyl glucoside series might help to design more active SGLT2 inhibitors that are structurally related.

CiteXplore: 20181486

DOI: 10.1016/j.bmc.2010.01.073