Synthesis, antioxidant and anticholinesterase activities of novel quinoline‐aminophosphonate derivatives,Journal of Heterocyclic Chemistry

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Synthesis, antioxidant and anticholinesterase activities of novel quinoline‐aminophosphonate derivatives
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-02-26 , DOI: 10.1002/jhet.3933
Ismahene Bazine ₁ , Zinelaabidine Cheraiet _{1,

2} , Rafik Bensegueni _{3,

4} , Chawki Bensouici ₅ , Abbes Boukhari ₁

Affiliation

A series of 20 novel α‐aminophosphonate derivatives bearing quinoline or quinolone moiety was designed and synthesized via Kabachnik‐Fields reaction in the presence of triethylammonium acetate as a solvent and catalyst under ultrasound irradiation. This procedure affords products in high yields and short reaction times. Molecular structures of the synthesized compounds 4a‐g and 5a‐m were confirmed using various spectroscopic methods. The antioxidant activity of these compounds was evaluated by eight complementary in vitro tests. The anticholinesterase activity (AChE, BChE) of these compounds were also evaluated. In addition, theoretical calculations of all compounds were investigated as corrosion inhibitors using density functional theory (DFT). The results revealed that 16 of these compounds exhibited high levels of antioxidant activities depending on the assay and that most compounds showed more potent inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).

中文翻译：

新型喹啉-氨基膦酸酯衍生物的合成，抗氧化剂和抗胆碱酯酶活性

在超声波辐射下，在乙酸三乙铵作为溶剂和催化剂的情况下，通过Kabachnik-Fields反应设计并合成了一系列20种带有喹啉或喹诺酮部分的新型α-氨基膦酸酯衍生物。该程序提供了高产率和短反应时间的产物。合成的化合物4a-g和5a-m的分子结构已通过各种光谱方法得以证实。通过八个互补的体外评估这些化合物的抗氧化活性测试。还评估了这些化合物的抗胆碱酯酶活性（AChE，BChE）。此外，使用密度泛函理论（DFT）研究了所有化合物作为缓蚀剂的理论计算。结果表明，根据测定方法，这些化合物中的16种表现出高水平的抗氧化活性，大多数化合物对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）表现出更强的抑制活性。

更新日期：2020-02-26

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