SYNTHESIS AND ANTIOXIDANT ACTIVITY OF SOME AMINOADAMANTANE DERIVATIVES

Antoniya Stoymirska, R. Chayrov, A. Georgieva, E. Tsvetanova, A. Alexandrova, I. Stankova
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Abstract

Chronic fatigue syndrome (CFS) and neurocognitive deficits are a major problem of modern society. The etiology of CFS remains unclear, however, a large number of recent studies have shown oxidative stress may be involved in its pathogenesis. Fatigue is frequent and important in the lives of Parkinson’s disease (PD) patients. 1-amino-adamantane (amantadine and memantine) derivatives has been proposed to be useful in the treatment of Parkinson’s and Alzheimer’s diseases. Its beneficial effect has been related to its novel properties as an N-methyl-D-aspartate receptor (NMDAR) blocker which can neutralize the effect of glutamate at striatal and subthalamic levels. We synthesized and evaluated the antioxidant activity of eleven new aminoadamantane derivatives. Their antioxidant activity has been evaluated using different (superoxide anion, hydroxyl) radical generating systems. The compoundwith s highest anti-oxidative capacity contain 2-(Benzhydrylsulfinyl) substituent.
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一些氨基金刚烷衍生物的合成和抗氧化活性
慢性疲劳综合征(CFS)和神经认知缺陷是现代社会的一个主要问题。慢性疲劳综合征的病因尚不清楚,但最近的大量研究表明,氧化应激可能与慢性疲劳综合征的发病机制有关。疲劳是帕金森病(PD)患者生活中经常出现的重要症状。1-氨基金刚烷(金刚烷胺和美金刚)衍生物被认为可用于治疗帕金森病和阿尔茨海默病。其有益效果与其作为 N-甲基-D-天冬氨酸受体(NMDAR)阻断剂的新特性有关,该阻断剂可中和谷氨酸在纹状体和丘脑下水平的作用。我们合成并评估了 11 种新的氨基金刚烷衍生物的抗氧化活性。我们使用不同的(超氧阴离子、羟基)自由基生成系统对它们的抗氧化活性进行了评估。抗氧化能力最强的化合物含有 2-(二苯甲基亚磺酰基)取代基。
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Journal of Chemical Technology and Metallurgy
Journal of Chemical Technology and Metallurgy Engineering-Industrial and Manufacturing Engineering
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1.40
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