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

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 adhered to each other and to a surface that gives them even more protection and resistance to 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 of 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.

Novel Double-Modified Colchicine Derivatives Bearing 1,2,3-Triazole: Design, Synthesis, and Biological Activity Evaluation

“…Among the presented derivatives, the most interesting seem to be compounds 30 and 34 with high SI values and low IC 50 values. Important compounds, in terms of biological properties, are also compound 8 (aminomethyltriazole) and its amides (29,31,33,35,36) and carbamates (37)(38)(39)(40)(41)43) along with esters of hydroxymethyltriazole (24−27). The results clearly indicate that the appropriate selection of the side chain on C4′ carbon of 7-triazole-10-N-methylaminocolchicine allows obtaining derivatives with increased therapeutic potential compared to that of unmodified colchicine 1 or doxorubicin and cisplatin.…”

“…In pantothenamides, the triazole isoster in the place of the amide moiety allowed not only to prevent degradation of the compounds but also enhanced their antiplasmatic effect, while in phenacetin conjugates, in which the discussed moiety change allowed reduction of toxicity and at the same time led to improvement of the anti-inflammatory, antinociceptive, and antipyretic effects of unmodified phenacetin . It should also be mentioned that the compounds containing the 1,2,3-triazole skeleton in their structure exhibit a wide spectrum of biological properties such as antimicrobial, , anticancer, , antiviral, , anti-inflammatory, antitubercular, , or anti-Alzheimer’s disease …”