A quinoline-based FtsZ inhibitor for the study of antimicrobial activity and synergistic effects with β-lactam antibiotics

Zhiyuan Fang, Li Ban, Yanan Li, Wenchang Yuan, Zhihua Liu, Ting Liu, Xiaomei Li, Kwok yin Wong, Yujing Lu, Ning Sun, Xingang Yao

Research output: Journal article publicationJournal articleAcademic researchpeer-review

13 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)283-289
Number of pages7
JournalJournal of Pharmacological Sciences
Volume137
Issue number3
DOIs
Publication statusPublished - Jul 2018

Keywords

  • Antibacterial activity
  • Bacterial resistance
  • Cell division
  • FtsZ inhibitor
  • Synergistic effect

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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