Sammendrag
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 4–8 μg/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.
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