期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 10, 页码 2760-2764出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.02.069
关键词
methylenedisalicylic acid; PTP1B; obesity; protein tyrosine phosphatase; inhibitor
Methylenedisalicylic acid derivatives were synthesized and their inhibitory activities against protein tyrosine phosphalases (PTPases) examined. Two of the compounds, 8 and 9, showed K-i values of 9.4 and 6.3 mu M against PTP I B, 4- and 7-fold lower values compared to those against TC-PTP. They were reversible and slow-binding inhibitors against PTP I B. When compound 8 was fed to a mouse model, the weight gain and adipocyte fat storage induced by a high-fat-diet were significantly suppressed. (c) 2007 Elsevier Ltd. All rights reserved.
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