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新型4H-吡喃并[2,3-b]喹啉衍生物的合成及生物学评价,该衍生物可阻断乙酰胆碱酯酶和细胞钙信号,并对钙超载和自由基引起神经保护作用。

Synthesis and biological evaluation of new 4H-pyrano[2,3-b]quinoline derivatives that block acetylcholinesterase and cell calcium signals, and cause neuroprotection against calcium overload and free radicals.

作者信息

Marco-Contelles José, León Rafael, López Manuela G, García Antonio G, Villarroya Mercedes

机构信息

Laboratorio de Radicales Libres (IQOG, CSIC), C/Juan de la Cierva 3, 28006 Madrid, Spain.

出版信息

Eur J Med Chem. 2006 Dec;41(12):1464-9. doi: 10.1016/j.ejmech.2006.06.016. Epub 2006 Oct 6.

Abstract

The synthesis and biological evaluation of ethyl 5-amino-4-(3-pyridyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrano[2,3-b]quinoline-3-carboxylates (9-11) is described. We have found that these compounds inhibit AChE with a mild potency, mitigates the Ca(2+) triggered by high K(+), and cause neuroprotection against Ca(2+) overloading and free radical-induced neuronal death.

摘要

描述了5-氨基-4-(3-吡啶基)-2-甲基-6,7,8,9-四氢-4H-吡喃并[2,3-b]喹啉-3-羧酸乙酯(9-11)的合成及生物学评价。我们发现这些化合物以中等效力抑制乙酰胆碱酯酶,减轻高钾引发的[Ca(2+)]c,并对Ca(2+)过载和自由基诱导的神经元死亡具有神经保护作用。

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