First Report on Anti-TSWV Activities of Quinazolinone Derivatives Containing a Dithioacetal Moiety,Journal of Agricultural and Food Chemistry

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First Report on Anti-TSWV Activities of Quinazolinone Derivatives Containing a Dithioacetal Moiety
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-10-08 , DOI: 10.1021/acs.jafc.1c03171
Yuewen Liu ₁ , Jixiang Chen ₁ , Dandan Xie ₁ , Baoan Song ₁ , Deyu Hu ₁

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Tomato spotted wilt virus (TSWV) is a plant virus with strong infectivity and destructive power. Given the lack of effective control agents, TSWV causes significant economic damage to several vegetables and ornamental plants worldwide. In this study, we designed and synthesized a series of novel quinazolinone derivatives containing a dithioacetal moiety and evaluated their antiviral activity in vitro and in vivo against TSWV. Some candidate compounds showed good anti-TSWV activity. Compound 6n shows excellent anti-TSWV activity in vivo, and the EC₅₀ value is 188 mg/L, which is notably better than that observed for ribavirin (642 mg/L), xiangcaoliusuobingmi (420 mg/L), and ningnanmycin (257 mg/L). In addition, compound 6n interacts with TSWV coat protein at sites ARG94 and ARG95 forming four π-alkyl interactions. Compound 6n (9.4 μM) shows a better binding affinity with TSWV coat protein than ribavirin (67.8 μM), xiangcaoliusuobingmi (33.8 μM), and ningnanmycin (24.3 μM). Therefore, compound 6n can serve as a lead compound for the discovery of new antiviral agents for the management of TSWV.

中文翻译：

含有二硫缩醛部分的喹唑啉酮衍生物抗 TSWV 活性的首次报告

番茄斑萎病毒（TSWV）是一种具有较强传染性和破坏力的植物病毒。由于缺乏有效的控制剂，TSWV 对世界范围内的几种蔬菜和观赏植物造成了重大的经济损失。在这项研究中，我们设计并合成了一系列含有二硫缩醛部分的新型喹唑啉酮衍生物，并评估了它们在体外和体内对 TSWV的抗病毒活性。一些候选化合物显示出良好的抗 TSWV 活性。化合物6n在体内显示出优异的抗 TSWV 活性， EC ₅₀值为 188 mg/L，明显优于利巴韦林 (642 mg/L)、香草柳絮凝咪 (420 mg/L) 和宁南霉素 (257 mg/L)。此外，化合物6n在 ARG94 和 ARG95 位点与 TSWV 外壳蛋白相互作用，形成四个 π-烷基相互作用。化合物6n (9.4 μM) 与 TSWV 外壳蛋白的结合亲和力优于利巴韦林 (67.8 μM)、香草柳絮凝咪 (33.8 μM) 和宁南霉素 (24.3 μM)。因此，化合物6n可以作为先导化合物，用于发现治疗 TSWV 的新型抗病毒药物。

更新日期：2021-10-20

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