The larvicidal activity of natural inspired piperine-based dienehydrazides against Culex pipiens
Document Type
Article
Publication Title
Bioorganic Chemistry
Abstract
A series of piperine-based dienehydrazide derivatives were designed and synthesized to be used as insecticides against Culex pipiens. The chemical structure of compound 5n was confirmed by single-crystal x-ray diffraction. Their insecticidal activities of synthesized compounds were tested against third-instar larval of Cx. pipiens at concentrations ranging from 0.1 to 1.2 mg/mL. Among all derivatives, compounds 5a, 5b, 5f, 5g, 5m, 5n, 5o, 5p, and 5u displayed good activities. The final mortality rates at the concentration of 0.75 mg/mL after 48 h treatment, were found to be in the range from 80.00 to 83.33% and with LC50 values ranging from 0.221 to 0.094 mg/mL. These compounds demonstrated higher insecticidal activities than piperine and Deltamethrin (a commercial positive control). Molecular modelling reveals several molecular interactions between synthesized compounds and the substrate binding sits of acetylcholinesterase (AChE) that are predicted to be responsible for its binding and inhibition activity.
DOI
10.1016/j.bioorg.2019.103464
Publication Date
1-1-2020
Recommended Citation
Tantawy, Ahmed H.; Farag, Shaimaa M.; Hegazy, Lamees; Jiang, Hong; and Wang, Man Qun, "The larvicidal activity of natural inspired piperine-based dienehydrazides against Culex pipiens" (2020). Pharmaceutical and Administrative Sciences Faculty Publications. 91.
https://doi.org/10.1016/j.bioorg.2019.103464
https://collections.uhsp.edu/pharm-admin-sciences_pubs/91