Peptoid analogues of anoplin show antibacterial activity.
We have synthesised nine analogues of the antibacterial peptide anoplin with a peptoid residue at position 5 (H-GLLKXIKTLL-NH(2)). The most active compounds showed MIC-values of 12.5 and 25 microM against E.coli and S.aureus. These MIC-values are comparable with anoplin which showed 23 microM and 11 microM against E. coli and S.aureus. However, the selectivity was reversed. Our results indicate that peptoid analogues of anoplin are promising lead structures for developing new antibacterial agents.
IGM-Bioorganic Chemistry, Faculty of Life Sciences, University of Copenhagen, 1871 Frederiksberg C, Denmark. prh@life.ku.dk
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Meinike
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Hansen
D000595:Amino Acid Sequence; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D023181:Antimicrobial Cationic Peptides / Q000494:pharmacology*; D002942:Circular Dichroism; D004926:Escherichia coli / Q000187:drug effects*; D006461:Hemolysis; D006801:Humans; D008826:Microbial Sensitivity Tests; D034444:Peptoids / Q000138:chemical synthesis / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects*; D014862:Wasp Venoms / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D023181:Antimicrobial Cationic Peptides; D034444:Peptoids; D014862:Wasp Venoms; C443041:anoplin