1,4-二氢喹啉席夫碱的新型Β-lactams和噻唑烷酮衍生物:合成、抗菌活性和分子对接研究

IF 0.5 Q4 CHEMISTRY, MULTIDISCIPLINARY
H. Hrichi, Nadia Ali Ahmed Elkanzi, R. Bakr
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引用次数: 9

摘要

以新型希夫碱2a-c与氯乙酰氯和巯基乙酸为原料,成功地合成了一系列新的β-内酰胺类化合物3a-c和噻唑烷酮衍生物4a-c。通过不同的光谱技术,包括IR、1h和13c NMR、质谱和元素分析,确定了新化合物的化学结构。所得化合物对革兰氏阳性金黄色葡萄球菌、革兰氏阴性大肠杆菌、黄曲霉和白色念珠菌的体外抑菌活性进行了评价。所有化合物均表现出良好至优异的抑菌活性。此外,对合成的化合物进行分子对接研究,结果表明化合物3b和4b的结合亲和力与谷氨酸相当。这两种化合物都是抗菌和抗真菌药物,值得进一步研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel Β-lactams and Thiazolidinone Derivatives from 1,4-dihydroquinoxaline Schiff’s Base: Synthesis, Antimicrobial Activity and Molecular Docking Studies
A series of novel isolated β-lactams 3a-c and thiazolidinone derivatives 4a-c were successfully synthesized from reactions of new Schiff's bases 2a-c with chloroacetyl chloride and thioglycolic acid. The chemical structures of the new compounds were confirmed through different spectroscopic techniques including IR, 1 H and 13 C NMR, mass spectrometry and elemental analysis. The antimicrobial activity of the obtained compounds was assessed in vitro against gram-positive Staphylococcus aureus and gram-negative Escherichia coli bacteria and Aspergillus flavus and Candida albicans fungi. All compounds exhibited good to excellent antimicrobial activity against the tested strains. Furthermore, a molecular docking study was carried out for the synthesized compounds and the results indicated that compounds 3b and 4b display comparable binding affinity scores as that of glutamate. These two compounds are promising candidates as antibacterial and antifungal agents that would deserve further investigations.
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来源期刊
Chemistry Journal of Moldova
Chemistry Journal of Moldova CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
0.90
自引率
20.00%
发文量
8
审稿时长
12 weeks
期刊介绍: "Chemistry Journal of Moldova. General, Industrial and Ecological Chemistry" seeks to publish experimental or theoretical research results of outstanding significance and timeliness in all fields of Chemistry, including Industrial and Ecological Chemistry. The main goal of this edition is strengthening the Chemical Society of Moldova, following development of research in Moldovan chemical institutions and promotion of their collaboration with international chemical community. Manuscripts are welcome from all countries.
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