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An amphipathic cyclic tetrapeptide scaffold containing halogenated ß2,2 -amino acids with activity against multiresistant bacteria.
Paulsen, Marianne H; Karlsen, Eskil André; Ausbacher, Dominik; Anderssen, Trude; Bayer, Annette; Ochtrop, Philipp; Hedberg, Christian; Haug, Tor; Ericson Sollid, Johanna U; Strøm, Morten B.
Afiliación
  • Paulsen MH; Department of Pharmacy, Faculty of Health Sciences, UiT-The Arctic University of Norway, Tromsø, Norway.
  • Karlsen EA; Department of Pharmacy, Faculty of Health Sciences, UiT-The Arctic University of Norway, Tromsø, Norway.
  • Ausbacher D; Hospital Pharmacy of North Norway Trust, Tromsø, Norway.
  • Anderssen T; Department of Pharmacy, Faculty of Health Sciences, UiT-The Arctic University of Norway, Tromsø, Norway.
  • Bayer A; Department of Chemistry, UiT-The Arctic University of Norway, Tromsø, Norway.
  • Ochtrop P; Department of Chemistry, Umeå University, Umeå, Sweden.
  • Hedberg C; Department of Chemistry, Umeå University, Umeå, Sweden.
  • Haug T; Norwegian College of Fishery Science, Faculty of Biosciences, Fisheries and Economics, UiT-The Arctic University of Norway, Tromsø, Norway.
  • Ericson Sollid JU; Department of Medical Biology, Faculty of Health Sciences, UiT-The Arctic University of Norway, Tromsø, Norway.
  • Strøm MB; Department of Pharmacy, Faculty of Health Sciences, UiT-The Arctic University of Norway, Tromsø, Norway.
J Pept Sci ; 24(10): e3117, 2018 Oct.
Article en En | MEDLINE | ID: mdl-30112781
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-ß2,2 -Xaa-Lys) containing one lipophilic ß2,2 -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 ß-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 4-8 µg/mL and low haemolytic activity. The combination of high antimicrobial activity and low toxicity shows that these cyclic tetrapeptides containing lipophilic ß2,2 -amino acids form a valuable scaffold for designing novel antimicrobial agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Péptidos Cíclicos / Farmacorresistencia Bacteriana Múltiple / Antibacterianos Idioma: En Revista: J Pept Sci Asunto de la revista: BIOQUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Noruega Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Péptidos Cíclicos / Farmacorresistencia Bacteriana Múltiple / Antibacterianos Idioma: En Revista: J Pept Sci Asunto de la revista: BIOQUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Noruega Pais de publicación: Reino Unido