n -{3-[(4-甲基苯-1-磺酰)亚胺]-6-氧环己-1,4-二烯-1-基}芳基酰胺及其衍生物的生物活性

S. Konovalova, A. Avdeenko, V. Lubenets, O. Komarovska-Porokhnyavets, I. Yakymenko, E. Lysenko
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引用次数: 0

摘要

N-{3-[(4-甲基-1-磺酰)亚胺]-6-氧环己-1,4-二烯-1-基}芳基酰胺及其衍生物是由相应的N-(4-氧环己-2,5-二烯-1-基)芳基磺酰胺与N-氯酰胺反应合成的。采用固体营养培养基上琼脂扩散法对大肠杆菌67、金黄色葡萄球菌209-p、黄体分枝杆菌VKM B-868和假丝酵母菌VKM Y-70、黑曲霉VKM F-1119进行了生物活性研究。试验化合物的活性程度由微生物生长抑制区直径决定。通过在液体营养培养基中连续稀释该物质的方法确定了最低抑菌、杀菌和杀真菌浓度。在研究的浓度下,将物质扩散到固体营养培养基上的琼脂中的方法表明,这些化合物对细菌大肠杆菌、金黄色葡萄球菌、黄体分枝杆菌和真菌假丝酵母、黑曲霉的活性较低。试验培养的微生物生长抑制带直径小于15mm。通过在液体营养培养基中对该物质进行连续稀释的方法研究,发现它们具有杀菌和杀真菌的活性。N-{2-羟基-5-[(4-甲基苯-1-磺酰)氨基]苯基}苯甲酰胺对黄体分枝杆菌的最低抑菌浓度为31.2 μg/ml。N-{2-羟基-3-甲基-5-[(4-甲基-1-磺酰)氨基]苯基}苯酰胺对黑曲霉的最低抑菌浓度为31.2 μg/ml。N-{2-羟基-5-[(4-甲基苯-1-磺酰)氨基]苯基}苯甲酰胺对黄体分枝杆菌的最低杀菌浓度为62.5 μg/ml。N-{3-[(4-甲基苯-1-磺酰基)亚胺]-6-氧环己-1,4-二烯-1-基}苯酰胺和N-{2-羟基-3-甲基-5-[(4-甲基苯-1-磺酰基)氨基]苯基}苯酰胺对霉菌黑曲霉的最小杀真菌浓度为62.5 μg/ml。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
BIOLOGICAL ACTIVITY OF N-{3-[(4-METHYLBENZENE-1- SULFONYL)IMINO]-6-OXOCYCLOHEXA-1,4-DIEN-1-YL}ARYLAMIDES AND THEIR DERIVATIVES
N-{3-[(4-Methylbenzene-1-sulfonyl)imino]-6-oxocyclohexa-1,4-dien-1-yl}arylamides and their derivatives were synthesized by the reaction of the corresponding N-(4-oxocyclohexa-2,5-dien-1-ylidene)arylsulfonamides with N-chloramides. The biological activity of the synthesized compounds was studied on test cultures of Escherichia coli 67, Staphylococcus aureus 209-p, Mycobacterium luteum VKM B-868 and fungi Candida tenuis VKM Y-70, Aspergillus niger VKM F-1119 by the method of diffusion of substances into agar on a solid nutrient medium. The degree of activity of the test compounds was determined by the diameter of the zones of inhibition of growth of test cultures of microorganisms. The minimum inhibitory, bactericidal and fungicidal concentrations were determined by the method of serial dilutions of the substance in a liquid nutrient medium. At the studied concentration, the method of diffusion of substances into agar on a solid nutrient medium has shown that these compounds have low activity against bacteria Escherichia coli, Staphylococcus aureus, Mycobacterium luteum and fungi Candida tenuis, Aspergillus niger. The diameters of the zones of inhibition of growth of test cultures of microorganisms were less than 15 mm. In research by the method of serial dilutions of the substance in a liquid nutrient medium, they have been found to have bactericidal and fungicidal activity. The minimum inhibitory concentration of N-{2-hydroxy-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide was 31.2 μg/ml against bacteria Mycobacterium luteum. The minimum inhibitory concentration of N-{2-hydroxy-3-methyl-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide against fungi Aspergillus niger was 31.2 μg/ml. The minimum bactericidal concentration of N-{2-hydroxy-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide was 62.5 μg/ml against bacteria Mycobacterium luteum. Minimum fungicidal concentration of N-{3-[(4-methylbenzene-1-sulfonyl)imino]-6-oxocyclohexa-1,4-dien-1-yl}benzamide and N-{2-hydroxy-3-methyl-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide was 62.5 μg/ml in action to mold fungi Aspergillus niger.
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