Semiautomated Total Synthesis of the Cyclic Lipodepsipeptide Anikasin

Org Lett. 2025 Mar 21;27(11):2559-2563. doi: 10.1021/acs.orglett.5c00111. Epub 2025 Mar 10.

Abstract

The total synthesis of Pseudomonas-derived cyclic lipodepsipeptide anikasin was achieved. Using a depsipeptide building block and balanced protecting groups on the branching d-allo-Thr residue, the synthesis was established semiautomatically on a synthesizer. Buffered deprotections minimized side reactions and afforded synthetic anikasin and its enantiomer. Biological activity studies indicated that anikasin's mode of action is directly resulting from its physicochemical properties.

MeSH terms

  • Depsipeptides* / chemical synthesis
  • Depsipeptides* / chemistry
  • Depsipeptides* / pharmacology
  • Molecular Structure
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / chemistry
  • Pseudomonas / chemistry
  • Stereoisomerism

Substances

  • Depsipeptides
  • Peptides, Cyclic