Synthesis and biological activity of highly cationic dendrimer antibiotics

Harrison W. Vankoten, Wendy M. Dlakic, Robert Engel, Mary J. Cloninger

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

The development of pathogenic bacteria resistant to current treatments is a major issue facing the world today. Here, the synthesis and biological activity of fourth generation poly(amidoamine) dendrimers decorated with 1-hexadecyl-azoniabicylo[2.2.2]octane (C16-DABCO), a quaternary ammonium compound known to have antibacterial activity, are described. This highly cationic dendrimer antibiotic was tested against several Gram positive and Gram negative strains of pathogenic bacteria and exhibited activity against both. Higher activity toward the Gram positive strains that were tested was observed. After the antimicrobial activity was assessed, E. coli and B. cereus were subjected to a resistance selection study. This study demonstrated that a multivalent approach to antimicrobial design significantly reduces the likelihood of developing bacterial resistance. Highly cationic dendrimers were also used as pretreatment of a membrane to prevent biofilm formation.

Original languageEnglish (US)
Pages (from-to)3827-3834
Number of pages8
JournalMolecular pharmaceutics
Volume13
Issue number11
DOIs
StatePublished - Nov 7 2016
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2016 American Chemical Society.

Keywords

  • antibiotic
  • cationic
  • dendrimers
  • multivalency
  • quaternary ammonium compound

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