A Simple Procedure for Synthesis of Biological Active 4-oxo-4-(quinolin-8-yloxy)but-2-enoic acid

IF 0.5 Q4 CHEMISTRY, MULTIDISCIPLINARY

Eurasian Chemico-Technological Journal Pub Date : 2022-03-31 DOI:10.18321/ectj1148

V. Merkulov, A.I. Almazov, S. Kabiyeva, S. Mantler, V. Konshin

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引用次数: 0

Abstract

The article is devoted to research on the synthesis of hydroxyquinoline derivative based on 8-oxyquinoline and maleic anhydride. Analysis of available literature was carried out, some drugs were found that are produced based on hydroxyquinoline derivatives and have antiprotozoal, antimicrobial and antiseptic effects, used alone or in combination with other active substances. A technique has been developed for the synthesis of a new derivative in the medium of petroleum distillate using sulfuric acid as a catalyst. A water-soluble ester of 8-oxyquinoline and maleic acid was obtained in good yield (95%), the structure of which was established based on UV, IR and NMR spectroscopy. By analogy with other oxyquinoline derivatives and the results of prediction bioactivity in the PASS program, the obtained derivative may be characterized by antifungal (antiseborrheic) action. It was determined its antibacterial properties at a concentration of 20.0–10.0 mg/cm3 as well as a significant antioxidant activity which is a useful biological property to expand the range of its application.

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生物活性4-氧代-4-（喹啉-8-氧基）丁-2-烯酸的简单合成方法

本文研究了以8-羟基喹啉和马来酸酐为原料合成羟基喹啉衍生物。对现有文献进行了分析，发现一些药物是基于羟基喹啉衍生物生产的，具有抗原生动物、抗菌和防腐作用，单独使用或与其他活性物质联合使用。开发了一种以石油馏分为介质，以硫酸为催化剂合成新衍生物的技术。通过紫外光谱、红外光谱和核磁共振光谱确定了8-氧喹啉与马来酸的水溶性酯的结构，产率为95%。与其他氧喹啉衍生物和PASS程序中预测生物活性的结果类似，所获得的衍生物可以具有抗真菌（抗心律失常）作用。测定了其在20.0–10.0 mg/cm3浓度下的抗菌性能以及显著的抗氧化活性，这是扩大其应用范围的有用生物特性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Eurasian Chemico-Technological Journal CHEMISTRY, MULTIDISCIPLINARY-

CiteScore

1.10

自引率

20.00%

发文量

审稿时长

20 weeks

期刊介绍： The journal is designed for publication of experimental and theoretical investigation results in the field of chemistry and chemical technology. Among priority fields that emphasized by chemical science are as follows: advanced materials and chemical technologies, current issues of organic synthesis and chemistry of natural compounds, physical chemistry, chemical physics, electro-photo-radiative-plasma chemistry, colloids, nanotechnologies, catalysis and surface-active materials, polymers, biochemistry.