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.
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http://dx.doi.org/10.1016/j.bmcl.2013.03.031 | DOI Listing |
Pest Manag Sci
February 2025
Syngenta AG, Basel, Switzerland.
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 PDFJ Agric Food Chem
November 2024
College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China.
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 PDFJ 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 PDFJ Agric Food Chem
September 2024
State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, P. R. China.
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.
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