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Novel inhibitors of nitric oxide synthase with antioxidant properties.

机译:具有抗氧化特性的新型一氧化氮合酶抑制剂。

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摘要

We previously described a series of imidazole-based inhibitors substituted at N-1 with an arylethanone chain as interesting inhibitors of neuronal nitric oxide synthase (nNOS), endowed with good selectivity vs endothelial nitric oxide synthase (eNOS). As a follow up of these studies, several analogs characterized by the presence of substituted imidazoles or other mono or bicyclic nitrogen-containing heterocycles instead of simple imidazole were synthesized, and their biological evaluation as in vitro inhibitors of both nNOS and eNOS is described herein. Most of these compounds showed improved nNOS and eNOS inhibitory activity with respect to reference inhibitors. Selected compounds were also tested to analyze their antioxidant properties. Some of them displayed good capacity to scavenge free radicals and ability to reduce lipid peroxidation.
机译:我们先前描述了一系列在N-1处被芳基酮链取代的基于咪唑的抑制剂,作为神经元一氧化氮合酶(nNOS)的有趣抑制剂,与内皮型一氧化氮合酶(eNOS)相比具有良好的选择性。作为这些研究的后续,合成了以取代的咪唑或其他单环或双环含氮杂环而不是简单的咪唑为特征的几种类似物,并在此描述了它们作为nNOS和eNOS的体外抑制剂的生物学评价。这些化合物中的大多数相对于参考抑制剂显示出改善的nNOS和eNOS抑制活性。还测试了所选化合物以分析其抗氧化性能。它们中的一些显示出清除自由基的良好能力和减少脂质过氧化的能力。

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