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Synthesis of paenipeptin C' analogues employing solution-phase CLipPA chemistry.

Juliana T W TongIman KavianiniaScott A FergusonGregory M CookPaul W R HarrisMargaret A Brimble
Published in: Organic & biomolecular chemistry (2020)
We herein report the synthesis of analogues of the antimicrobial lipopeptide, paenipeptin C', by installing varying lipid moieties using thiol-ene CLipPA (Cysteine Lipidation on a Peptide or Amino Acid) chemistry. Biological evaluation against both Gram-negative and Gram-positive strains indicated that several analogues possessed potent broad-spectrum antimicrobial activity.
Keyphrases
  • gram negative
  • multidrug resistant
  • molecular docking
  • amino acid
  • structure activity relationship
  • escherichia coli
  • staphylococcus aureus
  • drug discovery
  • fatty acid
  • fluorescent probe
  • molecular dynamics simulations