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甘草酸衍生物作为甲型H1N1流感病毒抑制剂

Glycyrrhizic acid derivatives as influenza A/H1N1 virus inhibitors.

作者信息

Baltina Lidia A, Zarubaev Vladimir V, Baltina Lia A, Orshanskaya Iana A, Fairushina Alina I, Kiselev Oleg I, Yunusov Marat S

机构信息

Institute of Organic Chemistry Ufa Research Centre of Russian Academy of Sciences, 71, prospect Oktyabrya, Ufa 450054, Russian Federation.

Influenza Research Institute, Ministry of Health of Russia, 15/17, prof. Popov str., St. Peterburg 197376, Russian Federation.

出版信息

Bioorg Med Chem Lett. 2015 Apr 15;25(8):1742-1746. doi: 10.1016/j.bmcl.2015.02.074. Epub 2015 Mar 7.

Abstract

This Letter describes the synthesis and antiviral activity study of some glycyrrhizic acid (GL) derivatives against influenza A/H1N1/pdm09 virus in MDCK cells. Conjugation of GL with l-amino acids or their methyl esters, and amino sugar (d-galactose amine) dramatically changed its activity. The most active compounds were GL conjugates with aromatic amino acids methyl esters (phenylalanine and tyrosine) (SI=61 and 38), and S-benzyl-cysteine (SI=71). Thus modification of GL is a perspective route in the search of new antivirals, and some of GL derivatives are potent as anti-influenza A/H1N1 agents.

摘要

本信函描述了一些甘草酸(GL)衍生物在MDCK细胞中对甲型H1N1/pdm09流感病毒的合成及抗病毒活性研究。GL与L-氨基酸或其甲酯以及氨基糖(D-半乳糖胺)的共轭显著改变了其活性。活性最高的化合物是与芳香族氨基酸甲酯(苯丙氨酸和酪氨酸)(SI = 61和38)以及S-苄基-半胱氨酸(SI = 71)的GL共轭物。因此,GL的修饰是寻找新型抗病毒药物的一个有前景的途径,并且一些GL衍生物作为抗甲型H1N1药物具有强效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6222/7127794/3ed9c2f08679/fx1_lrg.jpg

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