Antimicrobial activity of peptidomimetics against multidrug-resistant Escherichia coli: a comparative study of different backbones.
Novel remedies in the battle against multidrug-resistant bacterial strains are urgently needed, and one obvious approach involves antimicrobial peptides and mimics hereof. The impact of α- and β-peptoid as well as β(3)-amino acid modifications on the activity profile against β-lactamase-producing  Escherichia coli  was assessed by testing an array comprising different types of cationic peptidomimetics obtained by a general monomer-based solid-phase synthesis protocol. Most of the peptidomimetics possessed high to moderate activity toward multidrug-resistant  E. coli  as opposed to the corresponding inactive peptides. Nevertheless, differences in hemolytic activities indicate that a careful choice of backbone design constitutes a significant parameter in the search for effective cationic antimicrobial peptidomimetics targeting specific bacteria.
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Rasmus D
RD
Jahnsen
Niels
N
Frimodt-Møller
Henrik
H
Franzyk
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D023181:Antimicrobial Cationic Peptides / Q000737:chemistry*; D002942:Circular Dichroism; D024901:Drug Resistance, Multiple, Bacterial; D004355:Drug Stability; D004755:Enterobacteriaceae / Q000187:drug effects / Q000302:isolation & purification; D004926:Escherichia coli / Q000187:drug effects* / Q000302:isolation & purification; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D057786:Peptidomimetics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017433:Protein Structure, Secondary; D060327:Solid-Phase Synthesis Techniques; D013329:Structure-Activity Relationship; D053835:Unilamellar Liposomes
D000900:Anti-Bacterial Agents; D023181:Antimicrobial Cationic Peptides; D057786:Peptidomimetics; D053835:Unilamellar Liposomes