Next Article in Journal
Potential of FTIR-Spectroscopy for Drugs Screening against Helicobacter pylori
Next Article in Special Issue
Xanthones Active against Multidrug Resistance and Virulence Mechanisms of Bacteria
Previous Article in Journal
Are Follow-Up Blood Cultures Useful in the Antimicrobial Management of Gram Negative Bacteremia? A Reappraisal of Their Role Based on Current Knowledge
Previous Article in Special Issue
The Role of Efflux Pumps in the Transition from Low-Level to Clinical Antibiotic Resistance
Article

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

1
Department of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, 6720 Szeged, Hungary
2
Department of Biochemistry and Microbiology, Faculty of Food and Biochemical Technology, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague, Czech Republic
3
Instituto de Química Orgánica General (IQOG-CSIC), Consejo Superior de Investigaciones Científicas, Juan de la Cierva 3, 28006 Madrid, Spain
*
Authors to whom correspondence should be addressed.
Received: 12 November 2020 / Revised: 2 December 2020 / Accepted: 10 December 2020 / Published: 11 December 2020
(This article belongs to the Special Issue The Role of Efflux Pump Inhibitor in Bacterial Multidrug 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, 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 in vitro. 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 S. aureus and one ketone-selenoester on Salmonella 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 Vibrio campbellii strains. View Full-Text
Keywords: selenoesters; Salmonella species; Staphylococcus aureus; Pseudomonas aeruginosa; biofilm; quorum sensing; multidrug resistance; antibacterial activity selenoesters; Salmonella species; Staphylococcus aureus; Pseudomonas aeruginosa; biofilm; quorum sensing; multidrug resistance; antibacterial activity
Show Figures

Figure 1

MDPI and ACS Style

Szemerédi, N.; Kincses, A.; Rehorova, K.; Hoang, L.; Salardón-Jiménez, N.; Sevilla-Hernández, C.; Viktorová, J.; Domínguez-Álvarez, E.; Spengler, G. Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance. Antibiotics 2020, 9, 896. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9120896

AMA Style

Szemerédi N, Kincses A, Rehorova K, Hoang L, Salardón-Jiménez N, Sevilla-Hernández C, Viktorová J, Domínguez-Álvarez E, Spengler G. Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance. Antibiotics. 2020; 9(12):896. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9120896

Chicago/Turabian Style

Szemerédi, Nikoletta, Annamária Kincses, Katerina Rehorova, Lan Hoang, Noemi Salardón-Jiménez, Clotilde Sevilla-Hernández, Jitka Viktorová, Enrique Domínguez-Álvarez, and Gabriella Spengler. 2020. "Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance" Antibiotics 9, no. 12: 896. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9120896

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop