Antibacterial activity of 3-methylbenzo[d]thiazol-methylquinolinium derivatives and study of their action mechanism

Ning Sun, Ruo Lan Du, Yuan Yuan Zheng, Qi Guo, Sen Yuan Cai, Zhi Hua Liu, Zhi Yuan Fang, Wen Chang Yuan, Ting Liu, Xiao Mei Li, Yu Jing Lu, Kwok Yin Wong

Research output: Journal article publicationJournal articleAcademic researchpeer-review

16 Citations (Scopus)

Abstract

The increasing incidence of multidrug resistant bacterial infection renders an urgent need for the development of new antibiotics. To develop small molecules disturbing FtsZ activity has been recognized as promising approach to search for antibacterial of high potency systematically. Herein. series of novel quinolinium derivatives were synthesized and their antibacterial activities were investigated. The compounds show strong antibacterial activities against different bacteria strains including MRSA, VRE and NDM-1 Escherichia coli. Among these derivatives. compound bearin. 4-fluorophenyl group (A2) exhibite. superior antibacterial activity and its MICs to the drug-resistant strains are found lower than those of methicillin and vancomycin. The biological results suggest that these quinolinium derivatives can disrupt the GTPase activity and dynamic assembly of FtsZ, and thus inhibit bacterial cell division and then cause bacterial cell death. These compounds deserve further evaluation for the development of new antibacterial agents targeting FtsZ.

Original languageEnglish
Pages (from-to)879-889
Number of pages11
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume33
Issue number1
DOIs
Publication statusPublished - 1 Jan 2018

Keywords

  • 3-methylbenzo[d]thiazol-methylquinolinium derivatives
  • antibacterial activity
  • Bacterial resistance
  • cell division
  • FtsZ inhibition

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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