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Updated: Aug 5, 2026
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Protocols for Testing the Toxicity of Novel Insecticidal Chemistries to Mosquitoes
Published on: February 13, 2019
Design, Synthesis, Characterization, Toxicological Effects, and Molecular Docking Insights of Some Novel Quinoline
Mokhtar A Abdul-Malik1, Adel M Kamal El-Dean2, Abdel Haleem M Hussein3
1Department of Chemistry, Faculty of Applied Science, Taiz University, P.O. Box: 6169, Taiz, Yemen.
ACS Omega
|August 1, 2026
Summary
Researchers synthesized novel thienoquinoline derivatives as potential insecticides. Compound 10b showed high efficacy against Aphis fabae, demonstrating promise for developing new pest control agents.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Insecticide Development
Background:
- The need for novel insecticidal agents is driven by resistance to existing pesticides and environmental concerns.
- Thienoquinoline derivatives represent a class of heterocyclic compounds with diverse biological activities.
- Exploring new chemical scaffolds is crucial for discovering effective and selective pest control solutions.
Purpose of the Study:
- To synthesize and characterize novel thieno-[2,3-b]-quinoline derivatives.
- To evaluate the insecticidal efficacy of these compounds against Aphis fabae.
- To investigate the binding interactions of potent derivatives with insect nicotinic acetylcholine receptors.
Main Methods:
- Synthesis of hydrazone, arylidene, and pyrano-[3,2-c]-thieno-[2,3-b]-quinoline derivatives from ethyl 3-aminothieno-[2,3-b]-quinoline-2-carboxylate.
- Characterization using FT-IR, NMR, and mass spectrometry.
- Insecticidal activity assessment via probit analysis to determine median lethal concentration (LC50) values against Aphis fabae nymphs and adults.
- Molecular docking studies against Aplysia californica acetylcholine-binding protein (AChBP) as a surrogate for insect nicotinic acetylcholine receptors.
Main Results:
- A series of novel thienoquinoline derivatives were successfully synthesized and characterized.
- Compound 10b (pyrano-[3,2-c]-thieno-[2,3-b]-quinoline) exhibited potent insecticidal activity (LC50: 0.117 mg/L for nymphs, 0.366 mg/L for adults), comparable to acetamiprid.
- Molecular docking revealed strong binding affinity of pyranothienoquinoline derivatives, especially 10b (-7.30 kcal/mol), to AChBP, involving hydrogen bonds and hydrophobic interactions.
Conclusions:
- The pyrano-[3,2-c]-thieno-[2,3-b]-quinoline scaffold is a promising core structure for developing new insecticides.
- Compound 10b demonstrates significant potential as a lead compound for novel, target-specific pest control agents.
- Further research into these derivatives could lead to effective strategies against agricultural pests.
