Antibacterial activity of substituted dibenzo[a,g]quinolizin-7-ium derivatives

Ajit Parhi, Songfeng Lu, Cody Kelley, Malvika Kaul, Daniel S. Pilch, Edmond J. Lavoie

Research output: Contribution to journalArticlepeer-review

28 Scopus citations

Abstract

Berberine is a substituted dibenzo[a,g]quinolizin-7-ium derivative whose modest antibiotic activity is derived from its disruptive impact on the function of the essential bacterial cell division protein FtsZ. The present study reveals that the presence of a biphenyl substituent at either the 2- or 12-position of structurally-related dibenzo[a,g]quinolizin-7-ium derivatives significantly enhances antibacterial potency versus Staphylococcus aureus and Enterococcus faecalis. Studies with purified S. aureus FtsZ demonstrate that both 2- and 12-biphenyl dibenzo[a,g]quinolizin-7-ium derivatives act as enhancers of FtsZ self-polymerization.

Original languageEnglish (US)
Pages (from-to)6962-6966
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number22
DOIs
StatePublished - Nov 15 2012

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Molecular Medicine
  • Molecular Biology
  • Biochemistry
  • Clinical Biochemistry
  • Pharmaceutical Science
  • Organic Chemistry

Keywords

  • Antibacterial
  • Dibenzo[a,g]quinolizinium
  • Enterococcus faecalis
  • FtsZ-targeting
  • Staphylococcus aureus

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