Quinoline-2-one derivatives as promising antibacterial agents against multidrug-resistant Gram-positive bacterial strains.
Antibacterial
Biofilm
MRSA
MRSE
Quinoline
Resistance
VRE
Journal
Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology]
ISSN: 1678-4405
Titre abrégé: Braz J Microbiol
Pays: Brazil
ID NLM: 101095924
Informations de publication
Date de publication:
Dec 2023
Dec 2023
Historique:
received:
15
03
2023
accepted:
15
09
2023
pmc-release:
13
10
2024
medline:
4
12
2023
pubmed:
13
10
2023
entrez:
13
10
2023
Statut:
ppublish
Résumé
This study describes the discovery of a variety of quinoline2-one derivatives with significant antibacterial action vs a spectrum of multidrug-resistant Gram-positive bacterial strains, especially methicillin-resistant Staphylococcus aureus (MRSA). Compounds 6c, 6l, and 6o exhibited significant antibacterial activity versus the Gram-positive bacterial pathogens evaluated. In comparison to the reference daptomycin, compound 6c demonstrated the most effective activity among the assessed derivatives, with MIC concentrations of 0.75 μg/mL versus MRSA and VRE and 2.50 μg/mL against MRSE. We also reported on these compounds' biofilm and dihydrofolate reductase inhibitory activities. Compound 6c showed the greatest antibiofilm action in a dose-dependent way and a substantial decrease of biofilm development in the MRSA ACL51 strain at concentrations of 0.5, 0.25, and 0.12 MIC, with reductions of 79%, 55%, and 38%, consecutively, whereas the corresponding values for vancomycin were 20%, 12%, and 9%. These findings imply that these quinoline compounds could be used to develop a new category of antibiotic representatives to prevent Gram-positive drug-resistant bacterial strains.
Identifiants
pubmed: 37831330
doi: 10.1007/s42770-023-01132-w
pii: 10.1007/s42770-023-01132-w
pmc: PMC10689604
doi:
Substances chimiques
Anti-Bacterial Agents
0
Daptomycin
NWQ5N31VKK
Vancomycin
6Q205EH1VU
Quinolines
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2799-2805Informations de copyright
© 2023. The Author(s) under exclusive licence to Sociedade Brasileira de Microbiologia.
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