Discovery of a Novel Class of Acylthiourea-Containing Isoxazoline Insecticides against Plutella xylostella

Isoxazoline structures are widely found in natural products and are rich in biological activities. This study discloses the development of a series of novel isoxazoline derivatives by introducing acylthiourea fragments to access insecticidal activity. All synthetic compounds were examined for their...

Full description

Saved in:
Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2023-04, Vol.28 (8), p.3300
Main Authors: Li, Fangyi, Jiang, Biaobiao, Luo, Yuqin, He, Siqi, Feng, Di, Hu, Deyu, Song, Runjiang
Format: Article
Language:English
Subjects:
3D-QSAR
acylthiourea
Animals
Avermectin
Butterflies & moths
diamondback moth
Enzyme-linked immunosorbent assay
Enzymes
insecticidal activity
Insecticides
Insecticides - chemistry
Insecticides - pharmacology
Insects
isoxazoline
Larva
Mode of action
Molecular docking
Molecular Docking Simulation
Moths
Natural products
Optimization
Plutella xylostella
Proteomics
Quantitative Structure-Activity Relationship
Structure-Activity Relationship
γ-Aminobutyric acid
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Isoxazoline structures are widely found in natural products and are rich in biological activities. This study discloses the development of a series of novel isoxazoline derivatives by introducing acylthiourea fragments to access insecticidal activity. All synthetic compounds were examined for their insecticidal activity against , with results showing moderate to strong activity. Based on this, the structure-activity relationship analysis was carried out via the constructed three-dimensional quantitative structure-activity relationship model to further guide the structure optimization, resulting in the optimal compound . The LC of compound against was 0.26 mg/L, demonstrating better activity than the positive control, ethiprole (LC = 3.81 mg/L), avermectin (LC = 12.32 mg/L), and compounds - . The insect GABA enzyme-linked immunosorbent assay demonstrated that compound might act on the insect GABA receptor, and the molecular docking assay further illustrated the mode of action of compound with the GABA receptor. In addition, the proteomics analysis indicated that the action of compound on was multi-pathway.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules28083300