Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance

The emergence of drug-resistant pathogens leads to a gradual decline in the efficacy of many antibacterial agents, which poses a serious problem for proper therapy. Multidrug resistance (MDR) mechanisms allow resistant bacteria to have limited uptake of drugs, modification of their target molecules,...

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Bibliographic Details
Published in:Antibiotics (Basel) 2020-12, Vol.9 (12), p.896
Main Authors: Szemerédi, Nikoletta, Kincses, Annamária, Rehorova, Katerina, Hoang, Lan, Salardón-Jiménez, Noemi, Sevilla-Hernández, Clotilde, Viktorová, Jitka, Domínguez-Álvarez, Enrique, Spengler, Gabriella
Format: Article
Language:English
Subjects:
Antibacterial activity
Antibacterial agents
Antibacterial materials
Antibiotics
Antimicrobial activity
Bacteria
biofilm
Biofilms
Cell adhesion & migration
Communication
Deactivation
Derivatives
Efflux
Gram-negative bacteria
Inactivation
Ketones
Methicillin
Multidrug resistance
Multidrug resistant organisms
Oxidative stress
Pseudomonas aeruginosa
quorum sensing
Salmonella
Salmonella species
Selenium
selenoesters
Staphylococcus aureus
Staphylococcus infections
Viral infections
Virulence
Waterborne diseases
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Summary:The emergence of drug-resistant pathogens leads to a gradual decline in the efficacy of many antibacterial agents, which poses a serious problem for proper therapy. Multidrug resistance (MDR) mechanisms allow resistant bacteria to have limited uptake of drugs, modification of their target molecules, drug inactivation, or release of the drug into the extracellular space by efflux pumps (EPs). In previous studies, selenoesters have proved to be promising derivatives with a noteworthy antimicrobial activity. On the basis of these results, two series of novel selenoesters were synthesized to achieve more potent antibacterial activity on Gram-positive and Gram-negative bacteria. Fifteen selenoesters (eight ketone-selenoesters and seven cyano-selenoesters) were investigated with regards to their efflux pump-inhibiting, anti-quorum-sensing (QS), and anti-biofilm effects . According to the results of the antibacterial activity, the ketone-selenoesters proved to be more potent antibacterial compounds than the cyano-selenoesters. With regard to efflux pump inhibition, one cyano-selenoester on methicillin-resistant and one ketone-selenoester on Typhimurium were potent inhibitors. The biofilm inhibitory capacity and the ability of the derivatives to disrupt mature biofilms were noteworthy in all the experimental systems applied. Regarding QS inhibition, four ketone-selenoesters and three cyano-selenoesters exerted a noteworthy effect on strains.
ISSN:2079-6382
2079-6382
DOI:10.3390/antibiotics9120896