Al-Zharani Mohammed, Al-Eissa Mohammed S, Rudayni Hassan A, Ali Daoud, Alarifi Saud, SurendraKumar Radhakrishnan, Idhayadhulla Akbar
Biology Department, College of Science, Imam Mohammad Ibn Saud Islamic University, Riyadh 11623, Saudi Arabia.
Department of Zoology, College of Science, King Saud University, Riyadh 11461, Saudi Arabia.
Saudi J Biol Sci. 2022 Apr;29(4):2389-2395. doi: 10.1016/j.sjbs.2021.12.003. Epub 2021 Dec 10.
The pyrrolidine-2,4-dione derivatives were used to conduct a larvicidal test on 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 NMR, C NMR, mass spectrometry, and elemental analysis. Synthesized compounds () were evaluated for larvicidal activities. Compound (LD: 26.06 µg/mL), and (LD: 26.89 µg/mL), and were notably more active against than permethrin (LD: 26.14 µg/mL). The docking studies also demonstrated that and 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.
使用吡咯烷 - 2,4 - 二酮衍生物对二龄幼虫进行杀幼虫试验。采用曼尼希碱缩合方法通过研磨法合成吡咯烷 - 2,4 - 二酮衍生物。反应条件温和，产率高。使用傅里叶变换红外光谱（FTIR）、氢核磁共振（¹H NMR）、碳核磁共振（¹³C NMR）、质谱和元素分析对合成的化合物进行分析。对合成的化合物（）进行杀幼虫活性评估。化合物（半数致死剂量：26.06 μg/mL）和（半数致死剂量：26.89 μg/mL），对[此处原文缺失目标生物名称]的活性明显高于氯菊酯（半数致死剂量：26.14 μg/mL）。对接研究还表明，在蚊虫气味结合蛋白（蛋白质数据银行ID：3OGN）中，和是具有比对照更高结合能（-12.6千卡/摩尔）的强效杀幼虫剂。先导分子的杀幼虫特性使其成为重要的杀虫剂。
