Antimicrobial activity of various 4-and 5-substituted 1-phenylnaphthalenes

作者:Kelley Cody; Lu Songfeng; Parhi Ajit; Kaul Malvika; Pilch Daniel S; LaVoie Edmond J*
来源:European Journal of Medicinal Chemistry, 2013, 60: 395-409.
DOI:10.1016/j.ejmech.2012.12.027

摘要

Bacterial cell division occurs in conjunction with the formation of a cytokinetic Z-ring structure comprised of FtsZ subunits. Agents that can disrupt Z-ring formation have the potential, through this unique mechanism, to be effective against several of the newly emerging multi-drug resistant strains of infectious bacteria. 1- and 12-Aryl substituted benzo[c]phenanthridines have been identified as antibacterial agents that could exert their activity by disruption of Z-ring formation. Substituted 4- and 5-amino-1-phenylnaphthalenes represent substructures within the pharmacophore of these benzo[c] phenanthridines. Several 4- and 5-substituted 1-phenylnaphthalenes were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and Enterococcus faecalis. The impact of select compounds on the polymerization dynamics of S. aureus FtsZ was also assessed.

  • 出版日期2013-2