发现 Aldisine 及其衍生物作为新型抗病毒剂、杀幼虫剂和抗植物病原真菌剂,Journal of Agricultural and Food Chemistry

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发现 Aldisine 及其衍生物作为新型抗病毒剂、杀幼虫剂和抗植物病原真菌剂
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-09-21 , DOI: 10.1021/acs.jafc.2c04256
Wentao Xu ₁ , Rongxin Yang ₁ , Yanan Hao ₁ , Hongjian Song ₁ , Yuxiu Liu ₁ , Jingjing Zhang _{1,

2} , Yongqiang Li ₁ , Qingmin Wang ₁

Affiliation

基于氢键在药物设计中的广泛应用，设计合成了一系列含有肟、肟醚和腙部分的醛化衍生物，并首次评价了它们的抗病毒、杀幼虫和杀真菌活性。生物测定结果表明，这些衍生物中的大多数对烟草花叶病毒 (TMV) 具有活性。腙衍生物12在 500 mg/L时的体内灭活、治疗和保护活性分别为 52 ± 4、49 ± 1 和 52 ± 3%，与市售抗病毒药物宁南霉素 (57 ± 3, 56 ± 2 和 59 ± 1%）在相同剂量下。抗病毒机制研究表明，化合物12可引起20S CP（涂层蛋白）盘融合和解体，从而影响病毒颗粒的组装。分子对接结果表明化合物12与TMV CP之间存在明显的氢键。大多数衍生物对鳞翅目害虫的幼虫具有活性，例如Mythimna separata、Pyrausta nubilalis和Plutella xylostella。一些化合物还表现出对淡色库蚊的杀幼虫活性；其中化合物9和13的杀幼虫活性分别为 0.81 和 1.54 mg/L (LC ₅₀），分别。此外，大多数衍生物在50 mg/L时对14种植物病原真菌具有广谱杀菌活性。

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Discovery of Aldisine and Its Derivatives as Novel Antiviral, Larvicidal, and Antiphytopathogenic-Fungus Agents

Based on the widespread use of hydrogen bonds in drug design, a series of aldisine derivatives containing oxime, oxime ether, and hydrazone moieties were designed and synthesized, and their antiviral, larvicidal, and fungicidal activities were evaluated for the first time. The bioassay results showed that most of these derivatives were active against tobacco mosaic virus (TMV). Hydrazone derivative 12 showed in vivo inactivation, curative, and protection activities of 52 ± 4, 49 ± 1, and 52 ± 3% at 500 mg/L, which are comparable to that of the commercial antiviral drug ningnanmycin (57 ± 3, 56 ± 2, and 59 ± 1%, respectively) at the same dose. The antiviral mechanism study showed that compound 12 could cause 20S CP (coating protein) disk fusion and disintegration, thus affecting the assembly of virus particles. The result of molecular docking indicated that there were obvious hydrogen bonds between compound 12 and TMV CP. Most derivatives were active against larvae of lepidopteran pests, such as Mythimna separata, Pyrausta nubilalis, and Plutella xylostella. Some compounds also exhibited larvicidal activities against Culex pipiens; among them compounds 9 and 13 exhibited larvicidal activities of 0.81 and 1.54 mg/L (LC₅₀), respectively. Moreover, most of the derivatives showed broad-spectrum fungicidal activities against 14 kinds of phytopathogenic fungi at 50 mg/L.

更新日期：2022-09-21

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