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Biological evaluation of selected 1,2,3-triazole derivatives as antibacterial and antibiofilm agent.
Current Topics in Medicinal Chemistry ( IF 3.4 ) Pub Date : 2020-08-31 , DOI: 10.2174/1568026620666200710104737
Lialyz Soares Pereira André 1, 2 , Renata Freire Alves Pereira 1, 3 , Felipe Ramos Pinheiro 1, 2 , Aislan Cristina Rheder Fagundes Pascoal 4 , Vitor Francisco Ferreira 5 , Fernando de Carvalho da Silva 6 , Daniel Tadeu Gomes Gonzaga 7 , Dora Cristina Silva Costa 6 , Tainara Ribeiro 8 , Daniela Sachs 8 , Fábio Aguiar-Alves 1, 2, 4
Affiliation  

Background: Resistance to antimicrobial agents is a major public health problem, being Staphylococcus aureus prevalent in infections in hospital and community environments and, admittedly, related to biofilm formation in biotic and abiotic surfaces. Biofilms form a complex and structured community of microorganisms surrounded by an extracellular matrix adhering to each other and to a surface that gives them even more protection from and resistance against the action of antimicrobial agents, as well as against host defenses.

Methods: Aiming to control and solve these problems, our study sought to evaluate the action of 1,2,3- triazoles against a Staphylococcus aureus isolate in planktonic and in the biofilm form, evaluating the activity of this triazole through Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) tests. We have also performed cytotoxic evaluation and Scanning Electron Microscopy (SEM) of the biofilms under the treatment of the compound. The 1,2,3-triazole DAN 49 showed bacteriostatic and bactericidal activity (MIC and MBC 128 μg/mL). In addition, its presence interfered with the biofilm formation stage (1/2 MIC, p <0.000001) and demonstrated an effect on young preformed biofilm (2 MICs, p <0.05).

Results: Scanning Electron Microscopy images showed a reduction in the cell population and the appearance of deformations on the surface of some bacteria in the biofilm under treatment with the compound.

Conclusion: Therefore, it was possible to conclude the promising anti-biofilm potential of 1,2,3-triazole, demonstrating the importance of the synthesis of new compounds with biological activity.



中文翻译:

选定的1,2,3-三唑衍生物作为抗菌和抗生物膜剂的生物学评估。

背景:对抗菌剂的耐药性是一个主要的公共卫生问题,在医院和社区环境中普遍存在金黄色葡萄球菌,并且与生物和非生物表面生物膜的形成有关。生物膜形成了复杂而结构化的微生物群落,被彼此粘附并粘附于表面的细胞外基质所包围,从而赋予了它们更多的抗微生物剂作用以及抵抗宿主防御的保护力和抵抗力。

方法:为了控制和解决这些问题,我们的研究旨在评估1,2,3-三唑类对浮游生物和生物膜形式的金黄色葡萄球菌分离物的作用,并通过最小抑菌浓度(MIC)评估该三唑的活性。 )和最低杀菌浓度(MBC)测试。我们还对化合物处理下的生物膜进行了细胞毒性评估和扫描电子显微镜(SEM)。1,2,3-三唑DAN 49具有抑菌和杀菌活性(MIC和MBC 128μg/ mL)。此外,它的存在会干扰生物膜形成阶段(1/2 MIC,p <0.000001),并显示出对年轻的预制生物膜的影响(2 MIC,p <0.05)。

结果:扫描电子显微镜图像显示,在用该化合物处理后,生物膜中细胞数量减少,某些细菌表面出现变形。

结论:因此,有可能推断出有希望的1,2,3-三唑抗生物膜潜力,表明合成具有生物活性的新化合物的重要性。

更新日期:2020-11-02
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