首页> 外文期刊>EXCLI Journal >Synthesis and antibacterial activity of a new derivative of the meldrun acid: 2,2-dimethyl-5-(4H-1,2,4-triazol-4-ylaminomethylene)-1,3-dioxane-4,6-dione (C9H10N4O4)
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Synthesis and antibacterial activity of a new derivative of the meldrun acid: 2,2-dimethyl-5-(4H-1,2,4-triazol-4-ylaminomethylene)-1,3-dioxane-4,6-dione (C9H10N4O4)

机译:麦德龙酸新衍生物的合成及抗菌活性:2,2-二甲基-5-(4H-1,2,4-三唑-4-基氨基亚甲基)-1,3-二恶烷-4,6-二酮(C 9 H 10 N 4 O 4

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摘要

The discovery of new substances with proven antimicrobial activity is the current study goal of various researchers. Usage of synthetic products has grown considerably in the past few years due to processing agility, and capability of going through previous chemical modifications in order to enhance its biological activity. Widespread careless use of antimicrobials has made the number of resistant microorganisms rise significantly, thus demanding more efficient drugs to fight them. One of these synthetic candidates for this purpose is the substance 2,2-Dimethyl-5-(4H-1,2,4-triazol-4-ylaminomethylene)-1,3-dioxane-4,6-dione (C9H10N4O4), aminomethylene derivative from Meldrum's acid. This substance, alone and in association with common antibiotics, were evaluated in vitro for antimicrobial activity, and had their minimum inhibitory concentration (MIC) towards Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 10536 and Pseudomonas aeruginosa ATCC 15442, as well as multiresistant strains Escherichia coli 27, Staphylococcus aureus 358 and Pseudomonas aeruginosa 03 determined. The antimicrobial modulation action tests of the aminoglycosides with C9H10N4O4 were performed according to the microdilution method, and resulted in observation of a positive synergic effect.
机译:发现具有被证明具有抗菌活性的新物质是各种研究人员的当前研究目标。由于加工敏捷性以及经过先前化学修饰以增强其生物活性的能力,在过去几年中,合成产品的使用已大大增加。广泛使用粗心的抗菌药物已使耐药微生物的数量显着增加,因此需要更有效的药物来对抗它们。这些合成候选物中的一种是物质2,2-二甲基-5-(4H-1,2,4-三唑-4-基氨基亚甲基)-1,3-二恶烷-4,6-二酮(C9H10N4O4),麦德鲁姆酸的氨基亚甲基衍生物。对该物质单独或与常见抗生素结合使用,对其体外抗菌活性进行了评估,并且对金黄色葡萄球菌ATCC 25923,大肠杆菌ATCC 10536和铜绿假单胞菌ATCC 15442以及多重耐药菌株具有最小抑菌浓度(MIC)。确定了大肠杆菌27,金黄色葡萄球菌358和铜绿假单胞菌03。根据微量稀释法对氨基糖苷与C9H10N4O4进行了抗菌调节作用试验,观察到了积极的协同作用。

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