期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 22, 页码 9757-9763出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.09.066
关键词
Protein tyrosine phosphatase 1B; Diabetes; Aryl C-glycosyl compounds; Click chemistry; 1,4-Benzoquinone; 1,4-Naphthoquinone
资金
- CNRS
- ENS Cachan
- National Natural Science Foundation of China [20876045]
- Shanghai Science and Technology Community [074107018]
Protein tyrosine phosphatase 1B (PTP1B) has emerged as a promising target for type 2 diabetes. We have successfully synthesized dimeric acetylated and benzoylated beta-C-D-glucosyl and beta-C-D-galactosyl 1,4-dimethoxy benzenes or naphthalenes by click chemistry. These compounds were further transformed into the corresponding beta-C-D-glycosyl-1,4-quinone derivatives by CAN oxidation. The in vitro inhibition test showed that dimeric benzoylated beta-C-D-glycosyl 1,4-dimethoxybenzenes or 1,4-benzoquinones were good inhibitors of PTP1B (IC50: 0.62-0.88 mu M), with no significant difference between gluco and galacto derivatives. (C) 2008 Elsevier Ltd. All rights reserved.
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