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含阿魏酸酯磺酰胺部分的设计、合成、抗病毒生物活性及作用机制

Design, Synthesis, Antiviral Bioactivity, and Mechanism of the Ferulic Acid Ester-Containing Sulfonamide Moiety.

作者信息

Ren Xiaoli, Li Xiangyang, Yin Limin, Jiang Donghao, Hu Deyu

机构信息

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.

出版信息

ACS Omega. 2020 Jul 29;5(31):19721-19726. doi: 10.1021/acsomega.0c02421. eCollection 2020 Aug 11.

Abstract

Tobacco mosaic virus (TMV) has caused huge economic losses to tobacco, pepper, cucumber, and ornamental crops all over the world. However, few effective antiviral agents were developed and applied to control such plant disease. It is challenging to find an anti-TMV agent which is highly effective, less toxic, and environmentally friendly. In this work, a series of ferulic acid ester-containing sulfonamide moieties were designed and synthesized, and the antiviral activities of these compounds against TMV were evaluated. The anti-TMV biological activity test showed that the target compounds showed excellent anti-TMV activity and . In particular, compound has excellent anti-TMV activity at 500 μg/mL, which is higher than that of the control drug ribavirin. The preliminary mechanism research results showed that compound can obviously destroy the morphology of the virions to show excellent activity. The results show that the ferulic acid ester-containing sulfonamide moiety deserves further research and development.

摘要

烟草花叶病毒(TMV)已给世界各地的烟草、辣椒、黄瓜和观赏作物造成了巨大的经济损失。然而,开发并应用于防治此类植物病害的有效抗病毒剂却很少。找到一种高效、低毒且环保的抗TMV剂具有挑战性。在这项工作中,设计并合成了一系列含有阿魏酸酯的磺酰胺部分,并评估了这些化合物对TMV的抗病毒活性。抗TMV生物活性测试表明,目标化合物表现出优异的抗TMV活性。特别是,化合物在500μg/mL时具有优异的抗TMV活性,高于对照药物利巴韦林。初步机制研究结果表明,化合物可明显破坏病毒粒子的形态,从而表现出优异的活性。结果表明,含有阿魏酸酯的磺酰胺部分值得进一步研发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5631/7424737/2cbeb0877785/ao0c02421_0001.jpg

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