Synthesis of benzofuran scaffold-based potential PTP-1B inhibitors
Synthesis of benzofuran scaffold-based potential PTP-1B inhibitors
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DOI：
10.1016/j.bmc.2006.10.053
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发表时间：
2007-01-15
影响因子：
3.5
通讯作者：
Goel, Atul
中科院分区：
文献类型：
--
作者：
Dixit, Manish;Tripathi, Brajendra K.;Goel, Atul
蛋白酪氨酸磷酸酶113（PTP-1B）是一种通过胰岛素受体的去磷酸化在下调胰岛素信号传导中起关键作用的酶。研究表明，PTP-1B基因敲除小鼠在肌肉和肝脏中显示出增加的胰岛素敏感性以及对肥胖的抵抗力。一系列羟基苯并呋喃甲基酮及其天然模拟二聚体和线性和角呋喃查尔酮和黄酮已被评估为PTP-1B抑制剂。筛选出的化合物具有较好的抑制活性。(c)2006爱思唯尔有限公司保留所有权利。
Protein tyrosine phosphatase 113 (PTP-1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Studies have shown that PTP-1B knockout mice showed increased insulin sensitivity in muscle and liver as well as resistance to obesity. A series of hydroxy benzofuran methyl ketones and their naturally mimicking dimers and linear and angular furanochalcones and flavones have been evaluated as PTP-1B inhibitors. Screened compounds displayed good inhibitory activity. (c) 2006 Elsevier Ltd. All rights reserved.