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Pestic Biochem Physiol ; 201: 105841, 2024 May.
Article in English | MEDLINE | ID: mdl-38685257

ABSTRACT

This work evaluated the insecticidal, antifeedant and AChE inhibitory activity of compounds with eudesmane skeleton. The insecticidal activity was tested against larvae of Drosophila melanogaster and Cydia pomonella, the compounds 3 and 4 were the most active (LC50 of 104.2 and 106.7 µM; 82.0 and 84.4 µM, respectively). Likewise, the mentioned compounds were those that showed the highest acetylcholinesterase inhibitory activity, with IC50 of 0.26 ± 0.016 and 0.77 ± 0.016 µM, respectively. Enzyme kinetic studies, as well as molecular docking, show that the compounds would be non-competitive inhibitors of the enzyme. The antifeedant activity on Plodia interpunctella larvae showed an antifeedant index (AI) of 99% at 72 h for compounds 16, 27 and 20. The QSAR studies show that the properties associated with the polarity of the compounds would be responsible for the biological activities found.


Subject(s)
Acetylcholinesterase , Cholinesterase Inhibitors , Drosophila melanogaster , Insecticides , Larva , Molecular Docking Simulation , Quantitative Structure-Activity Relationship , Sesquiterpenes, Eudesmane , Animals , Insecticides/pharmacology , Insecticides/chemistry , Cholinesterase Inhibitors/pharmacology , Cholinesterase Inhibitors/chemistry , Larva/drug effects , Drosophila melanogaster/drug effects , Acetylcholinesterase/metabolism , Sesquiterpenes, Eudesmane/pharmacology , Sesquiterpenes, Eudesmane/chemistry , Moths/drug effects , Sesquiterpenes/pharmacology , Sesquiterpenes/chemistry
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