Isoxazole-containing neonicotinoids: Design, synthesis, and insecticidal evaluation

Bioorg Med Chem Lett. 2018 Feb 15;28(4):831-833. doi: 10.1016/j.bmcl.2017.06.046. Epub 2017 Jun 20.

Abstract

A series of novel isoxazole-containing neonicotinoids were synthesized from nitromethylene analogues and aromatic aldehydes in the presence of l-proline/K2CO3. Bioassays indicated that several synthesized compounds showed 40-70% mortality against brown planthopper (Nilaparvata lugens) under the concentration of 4mgL-1, higher than that of imidacloprid (20%). Against cowpea aphid (Aphis craccivora), the best activity of title compounds reached 90% at the concentration of 20mgL-1.

Keywords: Imidacloprid; Insecticidal activity; Isoxazole; Neonicotinoids; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aphids / drug effects
  • Biological Assay
  • Drug Design
  • Hemiptera / drug effects
  • Insecticides / chemical synthesis
  • Insecticides / chemistry
  • Insecticides / pharmacology*
  • Isoxazoles / chemical synthesis
  • Isoxazoles / chemistry
  • Isoxazoles / pharmacology*
  • Molecular Structure
  • Neonicotinoids / chemical synthesis
  • Neonicotinoids / chemistry
  • Neonicotinoids / pharmacology*
  • Nitro Compounds / pharmacology

Substances

  • Insecticides
  • Isoxazoles
  • Neonicotinoids
  • Nitro Compounds
  • imidacloprid