Title of article
Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners Original Research Article
Author/Authors
Junwon Lee، نويسنده , , Sung-Han Lee، نويسنده , , Hee Jeong Seo، نويسنده , , Eun-Jung Son، نويسنده , , Suk Ho Lee، نويسنده , , Myung Eun Jung، نويسنده , , MinWoo Lee، نويسنده , , Ho-Kyun Han، نويسنده , , Jeongmin Kim، نويسنده , , Jahyo Kang، نويسنده , , Jinhwa Lee، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
17
From page
2178
To page
2194
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 (IC50 = 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.
Keywords
SGLT , Thiadiazole , Dapagliflozin , Diabetes , Glucoside
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2010
Journal title
Bioorganic and Medicinal Chemistry
Record number
1307222
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