Isoxazoline insecticides have been shown to be potent blockers of insect GABA receptors with excellent activity on a broad pest range, including Lepidoptera and Hemiptera. Herein we report on the synthesis, biological activity and mode-of-action for a class of 4-heterocyclic aryl isoxazoline insecticides.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2013.03.031DOI Listing

Publication Analysis

Top Keywords

isoxazoline insecticides
12
4-azolylphenyl isoxazoline
4
insecticides acting
4
acting gaba
4
gaba gated
4
gated chloride
4
chloride channel
4
channel isoxazoline
4
insecticides potent
4
potent blockers
4

Similar Publications

Background: Isoxazolines inhibit γ-aminobutyric acid chloride channels in insects and acarids by binding to postsynaptic receptors. This prevents chloride influx, leading to depolarization/hyperexcitation, paralysis, and death. Here, we evaluated the potential utility of a novel isoxazoline, isocycloseram, against several urban insect pests.

View Article and Find Full Text PDF

Due to the long-term overuse of chemical pesticides, serious resistance and negative problems on human health and the ecological environment have appeared. To develop plant-product-based pesticide candidates, a series of novel andrographolide ester derivatives containing the isoxazoline skeleton were prepared at the C-3 position. Their pesticidal activities were evaluated against three typical pests such as Walker, Van der Goot, and Boisduval.

View Article and Find Full Text PDF

N318L Blocks the Interaction of Fluralaner but Not Broflanilide or Fipronil with the Insect GABA Receptor .

J Agric Food Chem

October 2024

Key Laboratory of Integrated Pest Management on Crops in East China, Ministry of Agriculture and Rural Affairs/Key Laboratory of Integrated Management of Crop Diseases and Pests, Education of Ministry, College of Plant Protection, Nanjing Agricultural University, Nanjing 210095, P. R. China.

Fluralaner is a novel insecticide targeting the ionotropic GABA receptor (GABAR) subunit, RDL. A recent study revealed that N316L, a substitution of asparagine (N) with leucine (L), in the second transmembrane (M2)-spanning region reduced the antagonist action of fluralaner on the housefly RDL (RDL) . To verify the impact of N316L , the corresponding mutation (N318L) in the fruitfly RDL (RDL) was constructed using CRISPR/Cas9 genome editing.

View Article and Find Full Text PDF

Design, Synthesis, and Insecticidal Activity of Isoxazoline Derivatives Incorporating an Acylhydrazine Moiety.

J Agric Food Chem

September 2024

State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, P. R. China.

Article Synopsis
  • * A series of new isoxazoline compounds with acylhydrazine were created and tested for insecticidal activity, with one compound showing superior effectiveness compared to commercial options.
  • * Research indicated that the acylhydrazine's presence enhances biological activity, and the compound potentially interacts with the GABA receptor in the target insects, suggesting it could be a strong candidate for agricultural pest control.
View Article and Find Full Text PDF

Design, synthesis, and evaluation of novel isoxazoline derivatives containing 2-phenyloxazoline moieties as potential insecticides.

Pestic Biochem Physiol

September 2024

State Key Laboratory of Green Pesticide, Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, College of Plant Protection, South China Agricultural University, Guangzhou, Guangdong 510642, People's Republic of China. Electronic address:

Isoxazoline insecticides have shown broad-spectrum insecticidal activity against a variety of insect pests. However, the high toxicity of isoxazoline compounds towards honeybees restricts their application in crop protection. To mitigate this issue, a series of isoxazoline derivatives containing 2-phenyloxazoline were designed and synthesized.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!