Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity |
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Authors: | Shrestha Suja Bhattarai Bharat Raj Chang Kyung Ja Lee Keun-Hyeung Cho Hyeongjin |
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Affiliation: | Department of Chemistry and Institute of Molecular Cell Biology, Inha University, 253 Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea. |
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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. |
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