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

Org Biomol Chem. 2020 May 29. doi: 10.1039/d0ob00950d. Online ahead of print.


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.