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Updated: Jan 27, 2026

Synthesis of pH Dependent Pyrazole, Imidazole, and Isoindolone Dipyrrinone Fluorophores using a Claisen-Schmidt Condensation Approach
Published on: June 10, 2021
Novel Approaching Imidazoles as Insecticidal Agents: Design, Synthesis, Toxicological, Biochemical, and Biological
Norah A Alsaiari1, Amer A Amer2, Antar A Abdelhamid3
1Department of Chemistry, College of Science and Art, Najran University, Najran, Saudi Arabia.
Novel imidazoles incorporating ciprofloxacin show potent insecticidal activity against cotton leafworm larvae. Compound 6 is the most effective, impacting larval development and biochemical processes.
Area of Science:
- Synthetic organic chemistry
- Agricultural entomology
- Medicinal chemistry
Background:
- Insect resistance to existing pesticides is a growing global challenge.
- Development of novel insecticides with improved efficacy and safety profiles is crucial.
- Ciprofloxacin, an antibiotic, serves as a scaffold for new insecticidal compounds.
Purpose of the Study:
- To synthesize novel imidazole derivatives containing ciprofloxacin moieties.
- To evaluate the insecticidal activity of these compounds against Spodoptera littoralis.
- To investigate the impact of these compounds on various biological and biochemical parameters.
Main Methods:
- One-pot synthesis of imidazoles (3a-f) and pyrazoles (11, 12) using ciprofloxacin, formaldehyde, and heterocyclic derivatives.
- Insecticidal bioassays against second and fourth instar Spodoptera littoralis larvae.
- Assessment of effects on adult longevity, pupal development, fecundity, and egg hatchability.
- Biochemical analysis of key enzymes (acetylcholinesterase, ATPase, GST, CaE) and total protein in treated larvae.
Main Results:
- All synthesized compounds exhibited insecticidal efficacy against Spodoptera littoralis larvae.
- Compound 6 demonstrated the highest toxicity with an LC50 of 4.55 mg/L against second instar larvae.
- Significant alterations in biochemical parameters including enzyme activities and total protein were observed upon treatment with compound 6.
- Adverse effects on adult emergence, longevity, and fecundity were noted.
Conclusions:
- Novel imidazole derivatives incorporating ciprofloxacin show significant promise as effective insecticides.
- Compound 6 represents a potent lead candidate for managing insect resistance.
- Further research into the mechanism of action and optimization of these compounds is warranted.
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