Methylenedisalicylic acid derivatives: New PTP1B inhibitors that confer resistance to diet-induced obesity

S Shrestha, BR Bhattarai, KJ Chang, KH Lee…

文献索引：Shrestha, Suja; Bhattarai, Bharat Raj; Chang, Kyung Ja; Lee, Keun-Hyeung; Cho, Hyeongjin Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 10 p. 2760 - 2764

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被引用次数: 26

摘要

Methylenedisalicylic acid derivatives were synthesized and their inhibitory activities against protein tyrosine phosphatases (PTPases) examined. Two of the compounds, 8 and 9, showed Ki values of 9.4 and 6.3 μM 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 ...