Synthesis and Anti-insect Activity of Triazole-Containing Amide Derivatives.

Area of Science:

• Agricultural Science
• Organic Chemistry
• Entomology

Background:

• Crop pests, particularly hemipteran insects, significantly threaten global food security.
• Flonicamid (FL) is a key insecticide, but resistance and environmental concerns necessitate novel alternatives.

Purpose of the Study:

• Synthesize novel flonicamid derivatives using an active substructure splicing strategy.
• Evaluate the insecticidal efficacy of these derivatives against major agricultural pests.

Main Methods:

• Chemical synthesis of flonicamid derivatives.
• Bioassays to determine LC50 values against Myzus persicae, Bemisia tabaci, and Tetranychus urticae.
• Molecular docking and ADMET predictions for lead compound identification.

Main Results:

• Compounds 3ea, 3fa, 3ga, and 5cab showed moderate activity against Bemisia tabaci.
• Compounds 3aa, 5gaa, and 5fab demonstrated significant insecticidal activity against Myzus persicae.
• Compound 5fab exhibited superior efficacy compared to the reference flonicamid (FL).
• Molecular docking indicated strong interactions with target residues, correlating with high insecticidal activity.

Conclusions:

• Novel flonicamid derivatives were successfully synthesized and evaluated.
• Compounds 3aa and 5fab show promise as lead candidates for developing new, effective insecticides.
• Further research is warranted to optimize these candidates for agricultural applications.