The synthesis of cyclic tetrapeptoid analogues of the antiprotozoal natural product apicidin

Bioorg Med Chem Lett. 2001 Mar 26;11(6):773-6. doi: 10.1016/s0960-894x(01)00049-x.

Abstract

A novel synthetic strategy is described which may be used to prepare analogues of the antimalarial, fungal metabolite apicidin. Compared to the natural product, one analogue shows potent and selective activity in vitro against the parasite Trypanosoma brucei and low mammalian cell toxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Parasitic Sensitivity Tests
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacology
  • Trypanocidal Agents / chemical synthesis*
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / pharmacology
  • Trypanosoma brucei brucei / drug effects

Substances

  • Peptides, Cyclic
  • Trypanocidal Agents
  • apicidin