3-芳基胺甲基色素的抗菌活性

O. Khaeva, L. Ikoeva
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引用次数: 0

摘要

在微生物对最近使用的药物产生多重耐药的情况下,寻找具有明显的杀菌或抑菌作用、低毒性和致畸性的新化疗药物仍然是有意义的。色素衍生物具有广泛的药理活性(稳定膜、抗病毒、抗菌、抗炎、保护心脏、抗氧化),是研究新一代化疗药物的有前途的化合物。研究结果发现,革兰氏阳性菌金黄色葡萄球菌在液体营养培养基上生长时,对所研究的化合物表现出最高的敏感性。所研究的化合物对蜡样芽孢杆菌、大肠杆菌的致病性菌株也有活性。7-乙酰氧基-3-(对溴苯基)亚甲基铬的最小抑菌浓度为10 μg/ml, 3-(对溴苯基)亚甲基铬和7-乙酰氧基-3-(对磺胺苯基)亚甲基铬的最小抑菌浓度为20 μg/ml。7-乙酰氧基-3-(对溴苯基)亚甲基铬酮和3-(对溴苯基)亚甲基铬酮对芽孢形成菌枯草芽孢杆菌- MPC - 20 μg / ml具有较高的抑菌活性,合成的化合物对铜绿假单胞菌的抑菌活性较低。实验研究表明,3 -芳基氨基甲基色素结构中取代基的性质和位置影响其对革兰氏阳性菌金黄色葡萄球菌和革兰氏阴性菌大肠杆菌的枯草芽孢杆菌的抑菌活性。从磺胺类药物-去甲磺唑中合成了一系列抑菌活性与抗菌药物水平相当的3 -芳基氨基甲基色素化合物。
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ANTIBACTERIAL ACTIVITY OF 3-ARILYMINOMETHYLCHROMONES
In conditions of multiple drug resistance of microorganisms to recently used drugs, the search for new chemotherapeutic agents with a pronounced bactericidal or bacteriostatic effect with low toxicity and teratogenicity remains relevant. Chromone derivatives with a wide spectrum of pharmacological activity (membrane-stabilizing, antiviral, antibacterial, anti-inflammatory, cardioprotective, antioxidant) are promising compounds for the search for new generation chemotherapeutic drugs. As a result of the study, it was found that gram-positive bacteria Staphylococcus aureus shows the highest sensitivity to the studied compounds when growing on a liquid nutrient medium. The studied compounds are also active against pathogenic strains of Bacillus cereus, Escherichia coli. The minimum inhibitory concentration (IPC) of the most active substances in relation to St. strains aureus is 10 μg/ml for 7-acetoxy-3-(p-bromophenyl)iminomethylchromone, and for 3-(p-bromophenyl)-iminomethylchromone and 7-acetoxy-3-(p-sulfamidophenyl)iminomethylchromone – 20 μg/ml. For 7-acetoxy-3- (p-bromophenyl)iminomethylchromone and 3-(p-bromophenyl)iminomethylchromone, a high antibacterial activity was revealed with respect to the spore-forming bacteria Bacillus subtilis – MPC – 20 μg / ml. The synthesized compounds exhibit a low bacteriostatic activity with respect to the Pseudomonas aeruginosa strain. Experimental studies have shown that the nature and position of substituents in the structure of 3–aryliminomethylchromones affects their antibacterial activity against strains of gram-positive bacteria Staphulococcus aureus and Bacillus subtilis, a strain of gram-negative bacteria: Escherichia coli. The presence in the series of synthesized 3–aryliminomethylchromones of compounds with high bacteriostatic activity at the level of an antibacterial drug from the group of sulfonamides – norsulfazole was established.
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