Quaternized and Thiazole-Functionalized Free Radical-Generating Organometallic Dendrimers as Antimicrobial Platform against Multidrug-Resistant Microorganisms

Macromol Biosci. 2017 Jul;17(7). doi: 10.1002/mabi.201700020. Epub 2017 Mar 31.

Abstract

New macromolecules such as dendrimers are increasingly needed to drive breakthroughs in diverse areas, for example, healthcare. Here, the authors report hybrid antimicrobial dendrimers synthesized by functionalizing organometallic dendrimers with quaternary ammonium groups or 2-mercaptobenzothiazole. The functionalization tunes the glass transition temperature and antimicrobial activities of the dendrimers. Electron paramagnetic resonance spectroscopy reveals that the dendrimers form free radicals, which have significant implications for catalysis and biology. In vitro antimicrobial assays indicate that the dendrimers are potent antimicrobial agents with activity against multidrug-resistant pathogens such as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium as well as other microorganisms. The functionalization increases the activity, especially in the quaternary ammonium group-functionalized dendrimers. Importantly, the activities are selective because human epidermal keratinocytes cells and BJ fibroblast cells exposed to the dendrimers are viable after 24 h.

Keywords: antimicrobial; dendrimers; functionalization; multidrug-resistance; quaternization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents* / chemical synthesis
  • Anti-Infective Agents* / chemistry
  • Anti-Infective Agents* / pharmacology
  • Dendrimers* / chemical synthesis
  • Dendrimers* / chemistry
  • Dendrimers* / pharmacology
  • Drug Resistance, Multiple, Bacterial / drug effects*
  • Enterococcus faecium / growth & development*
  • Methicillin-Resistant Staphylococcus aureus / growth & development*
  • Organometallic Compounds* / chemical synthesis
  • Organometallic Compounds* / chemistry
  • Organometallic Compounds* / pharmacology
  • Thiazoles* / chemical synthesis
  • Thiazoles* / chemistry
  • Thiazoles* / pharmacology
  • Vancomycin Resistance / drug effects*

Substances

  • Anti-Infective Agents
  • Dendrimers
  • Organometallic Compounds
  • Thiazoles