Halogenation as a tool to tune antimicrobial activity of peptoids

Sci Rep. 2020 Sep 9;10(1):14805. doi: 10.1038/s41598-020-71771-8.

Abstract

Antimicrobial peptides have attracted considerable interest as potential new class of antibiotics against multi-drug resistant bacteria. However, their therapeutic potential is limited, in part due to susceptibility towards enzymatic degradation and low bioavailability. Peptoids (oligomers of N-substituted glycines) demonstrate proteolytic stability and better bioavailability than corresponding peptides while in many cases retaining antibacterial activity. In this study, we synthesized a library of 36 peptoids containing fluorine, chlorine, bromine and iodine atoms, which vary by length and level of halogen substitution in position 4 of the phenyl rings. As we observed a clear correlation between halogenation of an inactive model peptoid and its increased antimicrobial activity, we designed chlorinated and brominated analogues of a known peptoid and its shorter counterpart. Short brominated analogues displayed up to 32-fold increase of the activity against S. aureus and 16- to 64-fold against E. coli and P. aeruginosa alongside reduced cytotoxicity. The biological effect of halogens seems to be linked to the relative hydrophobicity and self-assembly properties of the compounds. By small angle X-ray scattering (SAXS) we have demontrated how the self-assembled structures are dependent on the size of the halogen, degree of substitution and length of the peptoid, and correlated these features to their activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / adverse effects
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Escherichia coli / drug effects
  • Halogenation
  • Humans
  • Microbial Sensitivity Tests
  • Peptoids / adverse effects
  • Peptoids / chemistry*
  • Peptoids / pharmacology*
  • Pseudomonas aeruginosa / drug effects
  • Scattering, Small Angle
  • Staphylococcus aureus / drug effects

Substances

  • Anti-Bacterial Agents
  • Peptoids