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Bioorg Med Chem. 2010 Mar 15;18(6):2178-2194. doi: 10.1016/j.bmc.2010.01.073. Epub 2010 Feb 4.

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

Author information

1
Central Research Laboratories, Green Cross Corporation, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
2
Department of Chemistry, Sogang University, 1 Shinsu-Dong, Mapo-Gu, Seoul 121-742, Republic of Korea.

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.

PMID:
20181486
DOI:
10.1016/j.bmc.2010.01.073
[Indexed for MEDLINE]

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