State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
J Agric Food Chem. 2020 May 13;68(19):5302-5308. doi: 10.1021/acs.jafc.0c00686. Epub 2020 Apr 29.
A series of novel quinazolinone sulfide derivatives containing a dithioacetal moiety were designed and synthesized using Tomato chlorosis virus coat protein (ToCVCP) as a potential drug target, and the inhibitory effect of ToCV was systematically evaluated in vitro and in vivo. The experimental results showed that most of the compounds presented a strong affinity. Notably, the binding abilities of compounds and to ToCVCP both reached a micromolar level, which were 0.19 and 0.83 μM, respectively. The relative expression level of ToCVCP gene was detected using real-time quantitative polymerase chain reaction in . Compounds and significantly reduced the relative expression level of ToCVCP gene by 93.34 and 83.47%, respectively, which were better than those of conventional antiviral agents. This study lays a good foundation for the structural design and modification of quinazolinone sulfide derivatives as anti-ToCV drugs.
设计并合成了一系列新型含二硫缩醛部分的喹唑啉酮硫化物衍生物，以番茄褪绿病毒外壳蛋白（ToCVCP）为潜在药物靶点，并在体外和体内系统评估了对 ToCV 的抑制作用。实验结果表明，大多数化合物表现出很强的亲和力。值得注意的是，化合物 和 与 ToCVCP 的结合能力均达到微摩尔水平，分别为 0.19 和 0.83 μM。使用实时定量聚合酶链反应检测 在 中的 ToCVCP 基因的相对表达水平。化合物 和 分别显著降低了 ToCVCP 基因的相对表达水平 93.34%和 83.47%，优于常规抗病毒药物。这项研究为作为抗 ToCV 药物的喹唑啉酮硫化物衍生物的结构设计和修饰奠定了良好的基础。
