Splicing Indoles and 4,5-Dihydro-1H-pyrazoline Structure Gave Birth to Novel Antiviral Agents: Design, Synthesis, and Mechanism Study,Journal of Agricultural and Food Chemistry

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Splicing Indoles and 4,5-Dihydro-1H-pyrazoline Structure Gave Birth to Novel Antiviral Agents: Design, Synthesis, and Mechanism Study
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2023-05-09 , DOI: 10.1021/acs.jafc.3c01005
Lian Bai ₁ , Chunle Wei ₁ , Zhongjie Shen ₁ , Hongfu He ₁ , Xiong Yang ₁ , Shaojie Shi ₁ , Deyu Hu ₁ , Baoan Song ₁

Affiliation

The specific conation of our research is to invent a series of indole derivatives containing a 4,5-dihydro-1H-pyrazoline motif with effective antiviral activity. The anti-potato virus Y (PVY) activities of target compounds were systematically investigated. Most target compounds exhibited good PVY activities. Compound D40, which exhibited outstanding anti-PVY activities, was sieved using a three-dimensional quantitative structure–activity relationship. Based on the anti-PVY activity assessments, the curative and protective activities of D40 were found to be 64.9 and 60.8%, respectively, which were superior to those of the commercial drug Ningnanmycin (50.2 and 50.7%, respectively). In addition, defensive enzyme activities and proteomics results indicate that D40 can increase the three crucial defense-related enzyme activities and regulate the carbon fixation pathway in photosynthetic organisms to intensify the resistance of plants to PVY. Therefore, our study suggests that compound D40 might be used as a suitable crop protection pesticide.

中文翻译：

拼接吲哚和 4,5-二氢-1H-吡唑啉结构催生新型抗病毒药物：设计、合成和机理研究

我们研究的具体构想是发明一系列具有有效抗病毒活性的4,5-二氢-1H-吡唑啉基序的吲哚衍生物。系统研究了目标化合物的抗马铃薯 Y 病毒 (PVY) 活性。大多数目标化合物表现出良好的 PVY 活性。使用三维定量结构-活性关系筛选显示出突出的抗 PVY 活性的化合物D40 。基于抗 PVY 活性评估，发现D40的治疗和保护活性分别为 64.9% 和 60.8%，优于商业药物宁南霉素（分别为 50.2% 和 50.7%）。此外，防御酶活性和蛋白质组学结果表明D40可以增加三种关键的防御相关酶活性，调节光合生物体内的固碳途径，增强植物对PVY的抗性。因此，我们的研究表明，化合物D40可作为一种合适的作物保护农药。

更新日期：2023-05-09

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