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Synthesis, molecular docking and PTP1B inhibitory activity of functionalized 4,5-dihydronaphthofurans and dibenzofurans.

机译:功能化的4,5-二氢萘呋喃和二苯并呋喃的合成,分子对接和PTP1B抑制活性。

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摘要

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.
机译:蛋白质酪氨酸磷酸酶1B(PTP1B)是一种在通过胰岛素受体的去磷酸化来下调胰岛素信号传导中起关键作用的酶。 PTP1B抑制剂表现出增加的胰岛素敏感性,并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4,5-二氢萘呋喃和二苯并呋喃,通过分子对接研究并评估了其对PTP1B的抑制活性。

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