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发现具有高抗病毒活性的新人参二醇类化合物。

Discovery of New Ginsenol-Like Compounds with High Antiviral Activity.

机构信息

Laboratory of Experimental Virology Pasteur Institute of Epidemiology and Microbiology, 14 Mira Str., 197101 St. Petersburg, Russia.

Department of Medicinal Chemistry, N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, Lavrentiev Ave. 9, 630090 Novosibirsk, Russia.

出版信息

Molecules. 2021 Nov 10;26(22):6794. doi: 10.3390/molecules26226794.

DOI:10.3390/molecules26226794
PMID:34833886
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8619001/
Abstract

A number of framework amides with a ginsenol backbone have been synthesized using the Ritter reaction. We named the acetamide as Ginsamide. A method was developed for the synthesis of the corresponding amine and thioacetamide. The new compounds revealed a high activity against H1N1 influenza, which was confirmed using an animal model. Biological experiments were performed to determine the mechanism of action of the new agents, a ginsamide-resistant strain of influenza virus was obtained, and the pathogenicity of the resistant strain and the control strain was studied. It was shown that the emergence of resistance to Ginsamide was accompanied by a reduction in the pathogenicity of the influenza virus.

摘要

已经使用里特反应合成了具有人参皂甙骨架的许多骨架酰胺。我们将乙酰胺命名为 Ginsamide。开发了一种合成相应胺和硫代乙酰胺的方法。这些新化合物在动物模型中证实对 H1N1 流感具有高活性。进行了生物实验以确定新试剂的作用机制,获得了对 Ginsamide 具有抗性的流感病毒株,并研究了抗性株和对照株的致病性。结果表明,对 Ginsamide 的抗性的出现伴随着流感病毒致病性的降低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/cf25db0fae4b/molecules-26-06794-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/cf25db0fae4b/molecules-26-06794-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/4bad671e938b/molecules-26-06794-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/a52df1bb7cf4/molecules-26-06794-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/330d554d1a8d/molecules-26-06794-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/ce1fcc51e4b9/molecules-26-06794-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/1cc1278d47a8/molecules-26-06794-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/8d0b0ca96967/molecules-26-06794-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/a8be49ce9d36/molecules-26-06794-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/c3308857f7f8/molecules-26-06794-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/6f905763a175/molecules-26-06794-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/203fc521ba82/molecules-26-06794-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/2890bf561ec9/molecules-26-06794-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/b68087561626/molecules-26-06794-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61af/8619001/cf25db0fae4b/molecules-26-06794-g011.jpg

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