Department of Molecular Biology, Institute of Biotechnology, The John Paul II Catholic University of Lublin, ul. Konstantynów 1i, 20-708 Lublin, Poland.
Organic Chemistry Department, Faculty of Chemistry, Maria Curie-Skłodowska University, ul. Gliniana 33, 20-614 Lublin, Poland.
Eur J Med Chem. 2016 Nov 29;124:1019-1025. doi: 10.1016/j.ejmech.2016.10.034. Epub 2016 Oct 17.
Naphthalene-1,4-dione derivatives were synthesized and tested against selected bacterial strains. All the tested compounds were prepared by direct introduction of corresponding substituents into the naphthoquinone core in oxidative conditions. In this study, eight strains of bacteria (Proteus, Escherichia, Klebsiella, Staphylococcus, Enterobacter, Pseudomonas, Salmonella, Enterococcus) were used for determination of antimicrobial activity of synthesized compounds with the Minimal Inhibitory Concentration (MIC) method. Additionally, selected compounds were tested for haemolytic activity using human erythrocytes. All naphthalene-1,4-dione derivatives exhibited significant antimicrobial activity with MIC values between 7.8 and 500 μg/ml. A majority of the synthesized compounds showed the strongest antibacterial properties towards S. aureus, with a high level of selectivity. None of the tested naphthalene-1,4-dione derivatives exhibited haemolytic activity.
萘-1,4-二酮衍生物被合成并针对选定的细菌菌株进行了测试。所有测试的化合物都是通过在氧化条件下将相应的取代基直接引入萘醌核中来制备的。在这项研究中，使用了八种细菌（变形杆菌、大肠杆菌、克雷伯菌、金黄色葡萄球菌、肠杆菌、假单胞菌、沙门氏菌、肠球菌），采用最小抑菌浓度（MIC）法测定合成化合物的抗菌活性。此外，还用人红细胞测试了选定的化合物的溶血活性。所有萘-1,4-二酮衍生物均表现出显著的抗菌活性，MIC 值在 7.8 和 500μg/ml 之间。大多数合成的化合物对金黄色葡萄球菌表现出最强的抗菌特性，具有很高的选择性。测试的萘-1,4-二酮衍生物均没有表现出溶血活性。
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