Antimicrobial Peptides Incorporating Halogenated Marine-Derived Amino Acid Substituents.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
08 Jun 2023
08 Jun 2023
Historique:
received:
15
03
2023
accepted:
01
05
2023
pmc-release:
08
06
2024
medline:
14
6
2023
pubmed:
14
6
2023
entrez:
14
6
2023
Statut:
epublish
Résumé
Small synthetic mimics of cationic antimicrobial peptides represent a promising class of compounds with leads in clinical development for the treatment of persistent microbial infections. The activity and selectivity of these compounds rely on a balance between hydrophobic and cationic components, and here, we explore the activity of 19 linear cationic tripeptides against five different pathogenic bacteria and fungi, including clinical isolates. The compounds incorporated modified hydrophobic amino acids inspired by motifs often found in bioactive marine secondary metabolites in combination with different cationic residues to probe the possibility of generating active compounds with improved safety profiles. Several of the compounds displayed high activity (low μM concentrations), comparable with the positive controls AMC-109, amoxicillin, and amphotericin B. A higher activity was observed against the fungal strains, and a low
Identifiants
pubmed: 37312845
doi: 10.1021/acsmedchemlett.3c00093
pmc: PMC10258904
doi:
Types de publication
Journal Article
Langues
eng
Pagination
802-809Informations de copyright
© 2023 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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