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ID: ALA1147909

Journal: Bioorg Med Chem Lett

Title: Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.

Authors: Shrestha S, Bhattarai BR, Chang KJ, Lee KH, Cho H.

Abstract: Methylenedisalicylic acid derivatives were synthesized and their inhibitory activities against protein tyrosine phosphatases (PTPases) examined. Two of the compounds, 8 and 9, showed K(i) values of 9.4 and 6.3microM against PTP1B, 4- and 7-fold lower values compared to those against TC-PTP. They were reversible and slow-binding inhibitors against PTP1B. 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.

CiteXplore: 17368023

DOI: 10.1016/j.bmcl.2007.02.069