4.5 Article

Mosquito larvicidal activity of pyrrolidine-2,4-dione derivatives: An investigation against Culex quinquefasciatus and molecular docking studies

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SAUDI JOURNAL OF BIOLOGICAL SCIENCES
卷 29, 期 4, 页码 2389-2395

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ELSEVIER
DOI: 10.1016/j.sjbs.2021.12.003

关键词

Mannich base; Pyrrolidine-2; 4-dione derivative; Grindstone chemistry; Larvicidal activity; Culex quinquefasciatus; Molecular docking

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  1. Deanship of Scientific Research at Imam Mohammad Ibn Saud Islamic University [RG-21-09-87]

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A larvicidal test was conducted on Culex quinquefasciatus larvae using pyrrolidine-2,4-dione derivatives. The synthesized compounds showed significant larvicidal activities and high binding energy.
The pyrrolidine-2,4-dione derivatives were used to conduct a larvicidal test on Culex quinquefasciatus larvae of the second instar. Mannich base condensation method was used to synthesis the pyrrolidine-2,4-dione derivatives by grindstone method. The reaction conditions were mild, resulting in high yields. An analysis of the synthesized compounds was carried out using FTIR, H-1 NMR, C-13 NMR, mass spectrometry, and elemental analysis. Synthesized compounds (1a-h) were evaluated for larvicidal activities. Compound 1e (LD50 : 26.06 mu g/mL), and if (LD50: 26.89 mu g/mL), and were notably more active against Culex quinquefasciatus than permethrin (LD50: 26.14 mu g/mL). The docking studies also demonstrated that 1e, and 1f are potent larvicides with higher binding energy (-12.6 kcal/mol) than the control in the mosquito odorant binding protein (PDB ID: 3OGN). The larvicidal properties of lead molecules have made them important for use as insecticides. (C) 2021 The Author(s). Published by Elsevier B.V. on behalf of King Saud University.

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