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

作者：Parhi Ajit; Lu Songfeng; Kelley Cody; Kaul Malvika; Pilch Daniel S; LaVoie Edmond J^*

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(22): 6962-6966.

DOI：10.1016/j.bmcl.2012.08.123

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

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.

• 出版日期2012-11-15