Discovery, synthesis, and insecticidal activity of cycloaspeptide E

J Nat Prod. 2006 Oct;69(10):1506-10. doi: 10.1021/np060219c.

Abstract

Several Penicillia and one Tricothecium strain produced a new, insecticidally active member of the cycloaspeptide family, with the proposed name cycloaspeptide E (1). The structure, which was determined on the basis of spectroscopic (NMR, UV, MS) data and Marfey amino acid analysis, was the tyrosine desoxy version of cycloaspeptide A (2). Two synthetic routes to compound 1 were developed: one a partial synthesis from 2 and the other a total synthesis from methyl alaninate hydrochloride. Cycloaspeptide E, the first member of this series not to contain a tyrosine moiety, is also the first to be reported with insecticidal activity.

MeSH terms

  • Animals
  • Ascomycota / chemistry*
  • Insecticides* / chemical synthesis
  • Insecticides* / chemistry
  • Insecticides* / isolation & purification
  • Insecticides* / pharmacology
  • Lepidoptera / drug effects*
  • Molecular Structure
  • Penicillium / chemistry*
  • Peptides, Cyclic* / chemistry
  • Peptides, Cyclic* / isolation & purification
  • Peptides, Cyclic* / pharmacology
  • Structure-Activity Relationship

Substances

  • Insecticides
  • Peptides, Cyclic
  • cycloaspeptide E