Synthesis and biological activity of novel macrocyclic antifungals: acylated conjugates of the ornithine moiety of the lipopeptidolactone FR901469

Bioorg Med Chem Lett. 2001 Feb 26;11(4):479-82. doi: 10.1016/s0960-894x(00)00705-8.

Abstract

A series of acylated analogues of the novel macrocyclic lipopeptidolactone FR901469 has been prepared and evaluated for antifungal and hemolytic activity. Several analogues displayed markedly reduced hemolytic potential and comparable protective effects to the natural product in a mouse model of candidiasis.

MeSH terms

  • Animals
  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / pharmacology
  • Candidiasis / drug therapy
  • Depsipeptides*
  • Hemolysis / drug effects
  • Mice
  • Mice, Inbred ICR
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / pharmacology
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Depsipeptides
  • FR 901469
  • Peptides, Cyclic