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An amphipathic cycl...
An amphipathic cyclic tetrapeptide scaffold containing halogenated β2,2-amino acids with activity against multiresistant bacteria
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Paulsen, Marianne H. (author)
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Karlsen, Eskil Andre (author)
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Ausbacher, Dominik (author)
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Anderssen, Trude (author)
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Bayer, Annette (author)
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- Ochtrop, Philipp (author)
- Umeå universitet,Kemiska institutionen
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- Hedberg, Christian (author)
- Umeå universitet,Kemiska institutionen
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Haug, Tor (author)
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Sollid, Johanna U. Ericson (author)
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Strøm, Morten B. (author)
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(creator_code:org_t)
- 2018-08-15
- 2018
- English.
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In: Journal of Peptide Science. - : John Wiley & Sons. - 1075-2617 .- 1099-1387. ; 24:10
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- The present study describes the synthesis and biological studies of a small series of head-to-tail cyclic tetrapeptides of the general structure c(Lys‐β2,2‐Xaa‐Lys) containing one lipophilic β2,2-amino acid and Lys, Gly, Ala, or Phe as the Xaa residue in the sequence. The peptides were investigated for antimicrobial activity against gram-positive and gram-negative reference strains and 30 multiresistant clinical isolates including strains with extended spectrum β-lactamase-carbapenemase (ESBL-CARBA) production. Toxicity was determined against human red blood cells. The most potent peptides showed high activity against the gram-positive clinical isolates with minimum inhibitory concentrations of 4-8μg/mL and low haemolytic activity. The combination of high antimicrobial activity and low toxicity shows that these cyclic tetrapeptides containing lipophilic β2,2-amino acids form a valuable scaffold for designing novel antimicrobial agents.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Keyword
- antimicrobial peptides
- beta-amino acids
- CARBA
- cyclic tetrapeptides
- ESBL
- MRSA
- multiresistant bacteria
- peptidomimetics
- SMAMPs
- synthetic mimics of antimicrobial peptides
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Paulsen, Mariann ...
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Karlsen, Eskil A ...
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Ausbacher, Domin ...
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Anderssen, Trude
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Bayer, Annette
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Ochtrop, Philipp
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show more...
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Hedberg, Christi ...
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Haug, Tor
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Sollid, Johanna ...
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Strøm, Morten B.
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
- Articles in the publication
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Journal of Pepti ...
- By the university
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Umeå University