功能化4,5-二氢萘并呋喃和二苯并呋喃的合成、分子对接及蛋白酪氨酸磷酸酶1B抑制活性
Synthesis, molecular docking and PTP1B inhibitory activity of functionalized 4,5-dihydronaphthofurans and dibenzofurans.
作者信息
Dixit Manish, Saeed Uzma, Kumar Amit, Siddiqi Mohammad Imran, Tamrakar Akhilesh K, Srivastava Arvind K, Goel Atul
机构信息
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
出版信息
Med Chem. 2008 Jan;4(1):18-24. doi: 10.2174/157340608783331515.
Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Inhibitors of PTP1B showed increased insulin sensitivity and normalize plasma glucose level and thus are useful therapeutic agents for the treatment of diabetes. A series of functionalized 4,5-dihydronaphthofurans and dibenzofurans were synthesized, studied through molecular docking and evaluated for their PTP1B inhibitory activity.
蛋白酪氨酸磷酸酶1B（PTP1B）是一种通过使胰岛素受体去磷酸化在下调胰岛素信号传导中起关键作用的酶。PTP1B抑制剂显示出胰岛素敏感性增加且使血浆葡萄糖水平正常化，因此是治疗糖尿病的有用治疗剂。合成了一系列功能化的4,5-二氢萘并呋喃和二苯并呋喃，通过分子对接进行研究并评估它们的PTP1B抑制活性。
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