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A quinoline-based FtsZ inhibitor for the study of antimicrobial activity and synergistic effects with β-lactam antibiotics
- Source :
- Journal of Pharmacological Sciences. 137:283-289
- Publication Year :
- 2018
- Publisher :
- Elsevier BV, 2018.
-
Abstract
- The antibacterial activity and the synergistic effect with β-lactam antibiotics of a new 1-methylquinolinium iodide derivative were investigated. The experimental results indicate that the compound possesses a strong antibacterial activity against a panel of bacteria including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli with the MIC values from 0.75 μg/mL to 6 μg/mL. In addition, this compound combined with β-lactam antibiotics shows strong synergistic antimicrobial activities against antibiotic-resistant strains of S. aureus. The results of biochemical studies also reveal that this compound can effectively disrupt GTPase activity, polymerization of FtsZ, and cell division to cause cell death. The compound shows high potential for further development as a new generation of antibacterial agents to fight against the emergence of multidrug-resistant bacteria.
- Subjects :
- Methicillin-Resistant Staphylococcus aureus
0301 basic medicine
medicine.drug_class
Antibiotics
beta-Lactams
medicine.disease_cause
beta-Lactamases
GTP Phosphohydrolases
Polymerization
Vancomycin-Resistant Enterococci
Microbiology
03 medical and health sciences
Antibiotic resistance
Bacterial Proteins
Drug Resistance, Bacterial
Escherichia coli
medicine
FtsZ
Pharmacology
Dose-Response Relationship, Drug
biology
Chemistry
Quinolinium Compounds
Drug Synergism
biology.organism_classification
Antimicrobial
Anti-Bacterial Agents
Cytoskeletal Proteins
030104 developmental biology
Staphylococcus aureus
biology.protein
Molecular Medicine
Antibacterial activity
Cell Division
Bacteria
Subjects
Details
- ISSN :
- 13478613
- Volume :
- 137
- Database :
- OpenAIRE
- Journal :
- Journal of Pharmacological Sciences
- Accession number :
- edsair.doi.dedup.....a913207d63482dec434455d812771813