亚甲基二水杨酸衍生物：赋予对饮食诱导性肥胖抗性的新型蛋白酪氨酸磷酸酶1B抑制剂。
Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.
作者信息
Shrestha Suja, Bhattarai Bharat Raj, Chang Kyung Ja, Lee Keun-Hyeung, Cho Hyeongjin
机构信息
Department of Chemistry and Institute of Molecular Cell Biology, Inha University, 253 Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2007 May 15;17(10):2760-4. doi: 10.1016/j.bmcl.2007.02.069. Epub 2007 Mar 3.
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.
合成了亚甲基二水杨酸衍生物，并检测了它们对蛋白酪氨酸磷酸酶（PTPases）的抑制活性。其中两种化合物，8号和9号，对PTP1B的K(i)值分别为9.4和6.3微摩尔，与对TC-PTP的值相比低4至7倍。它们是PTP1B的可逆性慢结合抑制剂。当将化合物8喂给小鼠模型时，高脂饮食诱导的体重增加和脂肪细胞脂肪储存得到了显著抑制。
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