Novel Avermectins Produced by Mutational Biosynthesis

J Antibiot (Tokyo). 1991 Mar;44(3):357-65. doi: 10.7164/antibiotics.44.357.

Abstract

Avermectins with a wide range of novel C-25 substituents have been prepared by feeding carboxylic acids or their biosynthetic precursors to a Streptomyces avermitilis mutant strain ATCC 53568. This organism lacks the ability to form isobutyric and S-2-methylbutyric acids from their 2-oxo acid precursors and thus is unable to produce natural avermectins unless supplied with these acids. The novel avermectins produced by mutational biosynthesis possess broad-spectrum antiparasitic activity.

MeSH terms

  • Animals
  • Anthelmintics / chemistry
  • Anthelmintics / metabolism*
  • Anthelmintics / pharmacology
  • Caenorhabditis / drug effects
  • Carboxylic Acids / metabolism
  • Chromatography, High Pressure Liquid
  • Diptera
  • Fermentation
  • Ivermectin / analogs & derivatives*
  • Ivermectin / chemistry
  • Ivermectin / metabolism
  • Ivermectin / pharmacology
  • Molecular Structure
  • Mutation
  • Streptomyces / genetics
  • Streptomyces / metabolism*

Substances

  • Anthelmintics
  • Carboxylic Acids
  • Ivermectin
  • avermectin