Design, Synthesis, and Bioactivity of Spiro Derivatives Containing a Pyridine Moiety
作者:Lijiao Yu、Shengxin Guo、Ya Wang、Anjing Liao、Wei Zhang、Ping Sun、Jian Wu
DOI:10.1021/acs.jafc.2c06189
日期:2022.12.21
We designed and synthesized a series of pyridine spiro derivatives and evaluated their insecticidal and antiviral activities. Some compounds exhibited good insecticidal and antiviral activities. Notably, the E series of compounds displayed good insecticidal activity against Tetranychus urticae. Compounds E20 (EC50 = 63.68 mg/L) and F4 (EC50 = 47.81 mg/L) exhibited inactivation activities against the
我们设计并合成了一系列吡啶螺环衍生物,并评估了它们的杀虫和抗病毒活性。一些化合物表现出良好的杀虫和抗病毒活性。值得注意的是,E系列化合物对Tetranychus urticae表现出良好的杀虫活性。化合物E20 (EC 50 = 63.68 mg/L) 和F4 (EC 50 = 47.81 mg/L) 对烟草花叶病毒 (TMV) 表现出灭活活性,这与宁南霉素 (EC 50 = 58.01 mg/L)相似. 分子对接表明化合物E20和F4对 TMV 外壳蛋白 (TMV-CP) 表现出令人满意的亲和力,其结合能(分别为-6.7 和-6.4 kcal/mol)略低于宁南霉素(-6.3 kcal/mol)。此外,分子动力学分析显示化合物E20和F4表现出比宁南霉素更好的结合稳定性值。微量热泳表明化合物E20 ( K d = 0.053 ± 0.016 μM) 和F4 ( K d = 0.045 ±