Biological Evaluation of Selected 1,2,3-triazole Derivatives as Antibacterial and Antibiofilm Agents

Author:

André Lialyz Soares Pereira1,Pereira Renata Freire Alves1,Pinheiro Felipe Ramos1,Pascoal Aislan Cristina Rheder Fagundes2,Ferreira Vitor Francisco3,de Carvalho da Silva Fernando4,Gonzaga Daniel Tadeu Gomes5,Costa Dora Cristina Silva4,Ribeiro Tainara6,Sachs Daniela6,Aguiar-Alves Fábio1

Affiliation:

1. Universidade Fluminense Federal, Molecular Epidemiology and Biotechnology Laboratory (LEMB), Rodolpho Albino University Laboratory (LURA), Niteroi-RJ, Brazil

2. Universidade Federal Fluminense, Department of Basic Sciences, Nova Friburgo Health Institute, Nova Friburgo-RJ, Brazil

3. Universidade Federal Fluminense, Department of Pharmaceutical Technology, Pharmacy School, Niteroi-RJ, Brazil

4. Universidade Federal Fluminense, Instituto de Quimica, Departamento de Quimica Organica, Niteroi-RJ, Brazil

5. Universidade Estadual da Zona Oeste, Rio de Janeiro-RJ, Brazil

6. Universidade Federal de Itajuba, Department of Physics and Chemistry, Institute of Exact Sciences, Itajuba-MG, Brazil

Abstract

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.

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,General Medicine

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