Novel thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents

Novel thiophene C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different types of thiophene derivatives were readily prepared. Among the compounds tested, ethylphenyl at the distal ring 71p showed the best in vitro inhibitory activity in this series to date (IC 50 = 4.47 nM) ag...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2011-10, Vol.19 (19), p.5813-5832
Main Authors: Lee, Suk Ho, Song, Kwang-Seop, Kim, Jong Yup, Kang, Misuk, Lee, Jun Sung, Cho, Seung-Hwan, Park, Hyun-Ju, Kim, Jeongmin, Lee, Jinhwa
Format: Article
Language:English
Subjects:
Benzhydryl Compounds
Biological and medical sciences
chemistry
Dapagliflozin
Diabetes
General and cellular metabolism. Vitamins
Glucoside
Glucosides - chemical synthesis
Glucosides - chemistry
Glucosides - pharmacology
hypoglycemic agents
Hypoglycemic Agents - chemical synthesis
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacology
Medical sciences
Pharmacology. Drug treatments
SGLT
Sodium-Glucose Transporter 2 - metabolism
Sodium-Glucose Transporter 2 Inhibitors
Structure-Activity Relationship
Thiophene
Thiophenes - chemical synthesis
Thiophenes - chemistry
Thiophenes - pharmacology
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Summary:Novel thiophene C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different types of thiophene derivatives were readily prepared. Among the compounds tested, ethylphenyl at the distal ring 71p showed the best in vitro inhibitory activity in this series to date (IC 50 = 4.47 nM) against SGLT2. Novel thiophene C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different types of thiophene derivatives were readily prepared. Among the compounds tested, ethylphenyl at the distal ring 71p showed the best in vitro inhibitory activity in this series to date (IC 50 = 4.47 nM) against SGLT2.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2011.08.014