Structure-related antifeedant activity of halolactones with a p-menthane system against the lesser mealworm, Alphitobius diaperinus Panzer

Pest Manag Sci. 2014 Jun;70(6):953-8. doi: 10.1002/ps.3634. Epub 2013 Sep 30.

Abstract

Background: Feeding deterrent activity of synthetic halogen lactones against larvae and adults of the lesser mealworm, Alphitobius diaperinus Panzer, in laboratory choice and no-choice tests was studied. The compounds were synthesised from racemic and enantiomerically enriched (ee = 91-98%) cis- and trans-piperitols, which were obtained from (±)-piperitone.

Results: Structure-activity relationship studies identified several synthetic halolactones with a very strong feeding deterrent activity. The most active were the enantiomeric chlorolactones with chiral centre configurations (1S,4S,5R,6R) and (1R,4R,5S,6S) and their racemic mixture. The racemic bromo- and iodolactones obtained from cis-piperitol and saturated lactones with a chiral centre configuration (1R,4S,6R) were also very good antifeedants in comparison with piperitone. Most of the studied compounds were better antifeedants against adults than against larvae-among the 21 compounds, only one bromolactone with a chiral centre configuration (1S,4R,5R,6R) was a weaker deterrent for adults.

Conclusion: Chemical transformation of the piperitone molecule by the introduction of a lactone function and a halogen atom strongly changed its antifeedant properties against the lesser mealworm. Optimum activity is dependent on the presence of a chlorine atom at C-5 of the cyclohexane ring. The activity of bromo- and iodolactones depended strongly on the chiral centre configuration and the halogen substituent.

Keywords: Alphitobius diaperinus; antifeedants; halolactones; lesser mealworm; p-menthane lactones; piperitone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Coleoptera / drug effects*
  • Cyclohexane Monoterpenes
  • Insecticides / chemistry
  • Insecticides / toxicity
  • Lactones / chemistry*
  • Lactones / toxicity*
  • Larva / drug effects*
  • Monoterpenes / chemistry
  • Structure-Activity Relationship

Substances

  • Cyclohexane Monoterpenes
  • Insecticides
  • Lactones
  • Monoterpenes
  • piperitone