Antibacterial evaluation and mode of action study of BIMQ, a novel bacterial cell division inhibitor

Biochem Biophys Res Commun. 2019 Jul 5;514(4):1224-1230. doi: 10.1016/j.bbrc.2019.05.086. Epub 2019 May 17.

Abstract

The worldwide spreading of antibiotic resistant bacteria is currently an extremely serious health risk and therefore to develop new antibiotics is an urgent need. In the present study, the antibacterial activity of a new indolyl quinolinium compound and its underline mechanism were investigated. The compound shows an outstanding antibacterial activity against the tested Gram-positive bacteria. The MIC values are in the range of 1-4 μg/mL. The elongation of B. subtilis cells indicates that the compound can inhibit cell division effectively. In addition, the biochemical studies prove that the compound is able to disrupt FtsZ polymerization effectively through a stimulatory mechanism. Furthermore, the compound can delay the development of drug resistance mutants.

Keywords: Antibacterial activity; Cell division; Drug resistance; FtsZ.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacillus subtilis / cytology
  • Bacillus subtilis / drug effects*
  • Cell Division / drug effects
  • Dose-Response Relationship, Drug
  • Drug Resistance, Bacterial / drug effects
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Quinolinium Compounds / chemical synthesis
  • Quinolinium Compounds / chemistry
  • Quinolinium Compounds / pharmacology*
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Quinolinium Compounds