Synthesis, Physicochemical Properties, and Biological Activities of 4-(S-Methyl- N-(2,2,2-Trifluoroacetyl)Sulfilimidoyl) Anthranilic Diamide

Molecules. 2019 Sep 23;24(19):3451. doi: 10.3390/molecules24193451.

Abstract

Novel anthranilic diamides with sulfilimidoyl and sulfoximidoyl functionalities were successfully prepared. Among newly-prepared organosulfur compounds, 3-bromo-1-(3-chloropyridin-2-yl)-N-(2-methyl-6-(methylcarbamoyl)-4-(methylthio)phenyl)-1H-pyrazole-5-carboxamide and (S,E)-3-bromo-1-(3-chloropyridin-2-yl)-N-(2-methyl-4-(S-methyl-N-(2,2,2-trifluoroacetyl)sulfinimidoyl)-6-(methylcarbamoyl)phenyl)-1H-pyrazole-5-carboxamide showed good levels of efficacy and a strong correlation between insecticidal activities and physical properties, respectively. In particular, available data indicated that the N-trifluoroacetyl sulfilimine moiety could be an appealing structural scaffold for the discovery of a new crop-protecting agent.

Keywords: anthranilic diamide; insecticide; sulfilimine; sulfoximine.

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Chromatography, Thin Layer
  • Diamide / chemistry*
  • Insecticides / chemical synthesis
  • Insecticides / pharmacology
  • Isoxazoles / chemistry*
  • Spodoptera / drug effects
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Insecticides
  • Isoxazoles
  • Diamide
  • anthranil