Synthesis and insecticidal activities of novel pyrazole oxime ether derivatives with different substituted pyridyl rings

Pest Manag Sci. 2014 Aug;70(8):1207-14. doi: 10.1002/ps.3672. Epub 2013 Dec 6.

Abstract

Background: Pyrazole oxime ether derivatives with different substituted pyridyl rings represent new types of compounds that possess good insecticidal and acarcidal activity against Aphis laburni Kaltenbach and Tetranychus cinnabarinus.

Results: In total, 82 novel pyrazole oxime ether derivatives were synthesized and identified by (1) H NMR, elemental analysis or high-resolution mass spectrometry, and their insecticidal and acarcidal activities were tested against A. laburni Kaltenbach and T. cinnabarinus. Bioassays showed that at a 200 mg L(-1) dosage, one-third of the compounds displayed high insecticidal activity against A. laburni Kaltenbach (> 90%), whereas most of of the compound II series exhibited excellent acarcidal activity against T. cinnabarinus (> 92%). Most compound II series exhibited good activity in both insecticidal and acarcidal tests. In addition, at a low concentration of 10 mg L(-1) , the insecticidal activity of compounds IB9 and IE4 exceeded 90%, and the acarcidal activity of compounds IIB1 and IIB2 was ≥ 95%.

Conclusion: Structure-activity relationships were also examined. Results suggested that the tert-butoxycarbonyl group, as well as the position between tert-butoxycarbonyl and the atom N of the pyridyl ring, were essential to obtaining the acarcidal activity of the title compounds.

Keywords: inhibitors of complex I; insecticidal and acarcidal activity; pyrazole oxime ether derivatives; structure-activity relationship; substituted pyridyl ring.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aphids / drug effects
  • Drug Design*
  • Ethers / chemical synthesis
  • Ethers / chemistry
  • Insecticides / chemical synthesis
  • Insecticides / chemistry
  • Insecticides / toxicity
  • Oximes / chemistry
  • Pesticides / chemical synthesis
  • Pesticides / chemistry
  • Pesticides / toxicity*
  • Pyrazoles / chemistry
  • Structure-Activity Relationship
  • Tetranychidae / drug effects

Substances

  • Ethers
  • Insecticides
  • Oximes
  • Pesticides
  • Pyrazoles