Xu Fangzhou, Guo Shengxin, Zhang Wei, Wang Yanyan, Wei Panpan, Chen Shunhong, Wu Jian
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, China.
Pest Manag Sci. 2022 Apr;78(4):1417-1427. doi: 10.1002/ps.6758. Epub 2021 Dec 29.
Devastating plant virus diseases leading to bad harvests and lower quality of crops have made feeding the beyond seven billion population a huge challenge. Nevertheless, growing resistance and cross resistance of crop protection agents have made this challenge harder. Therefore, an efficient crop protection agent with novel structure and mode of action showing higher efficiency and eco-friendly is urgently needed.
The coat protein (CP) of a virus is a potential target for the discovery of new antiviral agents. Antiviral molecules can inhibit infection by obstructing the assembly of virus particles. A series of novel phthalamide-like thiourea derivatives containing trifluoromethylpyridine was designed and synthesized. Most of the compounds exhibited good antiviral activity against tobacco mosaic virus (TMV). Compound 7b showed notable curative, protective and inactivation activities against TMV. Its inactivation half-maximal effective concentration (EC ) value (20.5 μg mL ) was better even than commercial ningnanmycin (23.2 μg mL ). Compound 7b also had stronger TMV-CP binding ability than ningnanmycin and destroyed the external shape of TMV particles and hindered the self-assembly of TMV-CP and TMV-RNA.
These phthalamide-like thiourea derivatives especially compound 7b containing trifluoromethylpyridine are potential lead compounds and inhibitors of TMV particle self-assembly. © 2021 Society of Chemical Industry.
毁灭性的植物病毒病导致作物歉收和品质下降，这使得养活全球七十多亿人口成为一项巨大挑战。然而，作物保护剂抗性的不断增强和交叉抗性使得这一挑战更加艰巨。因此，迫切需要一种具有新颖结构和作用方式、高效且环保的作物保护剂。
病毒的外壳蛋白（CP）是发现新型抗病毒剂的潜在靶点。抗病毒分子可通过阻碍病毒颗粒的组装来抑制感染。设计并合成了一系列含三氟甲基吡啶的新型邻苯二甲酰胺类硫脲衍生物。大多数化合物对烟草花叶病毒（TMV）表现出良好的抗病毒活性。化合物7b对TMV显示出显著的治疗、保护和钝化活性。其钝化半数有效浓度（EC）值（20.5μg/mL）甚至优于市售宁南霉素（23.2μg/mL）。化合物7b与TMV-CP的结合能力也强于宁南霉素，且破坏了TMV颗粒的外形，阻碍了TMV-CP与TMV-RNA的自组装。
这些邻苯二甲酰胺类硫脲衍生物，尤其是含三氟甲基吡啶的化合物7b，是潜在的先导化合物和TMV颗粒自组装抑制剂。©2021化学工业协会。
