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Fluorinated antimicrobial lysine-based peptidomimetics with activity against methicillin-resistant Staphylococcus

Natalia Molchanova1, Paul R Hansen1, Peter Damborg2

  • 1Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen, Denmark.

Journal of Peptide Science : an Official Publication of the European Peptide Society
|July 3, 2018
PubMed

Insights

Novel peptidomimetics show promise for treating methicillin-resistant Staphylococcus pseudintermedius (MRSP) infections in dogs. Modifications like fluorination and longer side chains enhance potency against MRSP without increasing toxicity.

Area of Science:

  • Veterinary Medicine
  • Microbiology
  • Medicinal Chemistry

Background:

  • Staphylococcus pseudintermedius is a common opportunistic pathogen in dogs, causing skin and ear infections.
  • The rise of methicillin-resistant S. pseudintermedius (MRSP) presents a significant challenge in companion animal health.
  • There is a critical need for new therapeutic agents to combat MRSP infections.

Purpose of the Study:

  • To explore structure-activity relationships of peptidomimetics against MRSP.
  • To investigate the impact of oligomer length, fluorination, end-group modification, and hydrophobic side chain length on antibacterial activity and hemolytic properties.

Main Methods:

  • Synthesis and testing of 37 peptidomimetic compounds.
  • Evaluation of antibacterial activity against MRSP and other bacterial strains (S. aureus, E. coli, P. aeruginosa).
  • Assessment of hemolytic properties and cell selectivity.

Main Results:

  • Fluorination and longer hydrophobic side chains increased compound potency against MRSP without significant increases in hemolysis.
  • Reducing peptidomimetic length from 12 to 8 residues maintained antibacterial activity against MRSP.
  • End-group modifications enhanced activity against S. aureus, E. coli, and P. aeruginosa but also increased hemolytic properties, lowering cell selectivity.

Conclusions:

  • Optimized peptidomimetics, particularly those with fluorination and elongated hydrophobic chains, offer a promising avenue for treating MRSP infections in dogs.
  • Peptidomimetic length can be reduced for MRSP targeting, potentially simplifying drug design.
  • Further research is needed to balance efficacy and safety, especially concerning end-group modifications and hemolytic effects.
Keywords:
Staphylococcus pseudintermediusantimicrobialfluorinationpeptidomimetics

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