Sampaio Gillena M M, Teixeira Alexandre M R, Coutinho Henrique D M, Sena Junior Diniz M, Freire Paulo T C, Bento Ricardo R F, Silva Luiz E
Mestrado em Bioprospecção Molecular.
Mestrado em Bioprospecção Molecular ; Departamento de Física.
EXCLI J. 2014 Sep 1;13:1022-8. eCollection 2014.
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.
发现具有已证实抗菌活性的新物质是当前众多研究人员的研究目标。由于加工灵活性以及能够进行先前的化学修饰以增强其生物活性，合成产品的使用在过去几年中大幅增长。抗菌剂的广泛滥用使得耐药微生物的数量显著增加，因此需要更有效的药物来对抗它们。用于此目的的这些合成候选物之一是2,2 - 二甲基 - 5 -（4H - 1,2,4 - 三唑 - 4 - 基氨基亚甲基）-1,3 - 二氧六环 - 4,6 - 二酮（C9H10N4O4），麦氏酸的氨基亚甲基衍生物。该物质单独以及与常用抗生素联合，在体外评估其抗菌活性，并测定了它们对金黄色葡萄球菌ATCC 25923、大肠杆菌ATCC 10536和铜绿假单胞菌ATCC 15442以及多重耐药菌株大肠杆菌27、金黄色葡萄球菌358和铜绿假单胞菌03的最低抑菌浓度（MIC）。根据微量稀释法进行了C9H10N4O4与氨基糖苷类药物的抗菌调节作用测试，结果观察到正协同效应。
