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含1,2,3-三唑部分的尿苷糖缀合物的抗冠状病毒活性

Anticoronavirus Activity of Uridine Glycoconjugates Containing a 1,2,3-Triazole Moiety.

作者信息

Graul Malgorzata, Brzuska Gabriela, Wisniewska Ewa, Dominska Monika, Strakova Petra, Ruzek Daniel, Pastuch-Gawolek Gabriela, Krol Ewelina

机构信息

Laboratory of Recombinant Vaccines, Intercollegiate Faculty of Biotechnology, University of Gdansk and Medical University of Gdansk, Abrahama 58, Gdansk 80-307, Poland.

Laboratory of Virus Molecular Biology, Intercollegiate Faculty of Biotechnology, University of Gdansk and Medical University of Gdansk, Abrahama 58, Gdansk 80-307, Poland.

出版信息

J Med Chem. 2025 Aug 28;68(16):17859-17873. doi: 10.1021/acs.jmedchem.5c01602. Epub 2025 Aug 8.

Abstract

Coronaviruses can spread rapidly to new host species and cause severe respiratory and enteric diseases in vertebrates, including humans. To date, seven coronaviruses have been identified in humans, with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) being the most notorious due to its substantial social and economic impact. Although anti-SARS-CoV-2 vaccines are available, infections remain widespread, highlighting the ongoing need for antiviral treatments. Here, we report the synthesis and evaluation of the activity of uridine glycoconjugates, designed as glycosyltransferase donor-type inhibitors incorporating a 1,2,3-triazole moiety. These compounds were tested against two model coronaviruses: murine hepatitis virus strain A59 (MHV) and human coronavirus strain NL63 (HCoV-NL63). Four of the synthesized compounds demonstrated strong antiviral activity against both viruses, and their efficacy was further confirmed against SARS-CoV-2. Our results suggest that these compounds interfere with the coronavirus infectivity and replication process. Thus, these novel compounds may prove to be effective broad-spectrum antiviral inhibitors.

摘要

冠状病毒可迅速传播至新的宿主物种,并在包括人类在内的脊椎动物中引发严重的呼吸道和肠道疾病。迄今为止,已在人类中鉴定出七种冠状病毒,其中严重急性呼吸综合征冠状病毒2(SARS-CoV-2)因其巨大的社会和经济影响而最为臭名昭著。尽管已有抗SARS-CoV-2疫苗,但感染仍广泛存在,这凸显了对抗病毒治疗的持续需求。在此,我们报告了尿苷糖缀合物的合成及其活性评估,这些化合物被设计为含有1,2,3-三唑部分的糖基转移酶供体型抑制剂。这些化合物针对两种模型冠状病毒进行了测试:鼠肝炎病毒A59株(MHV)和人冠状病毒NL63株(HCoV-NL63)。四种合成化合物对这两种病毒均表现出强大的抗病毒活性,并且它们对SARS-CoV-2的疗效得到了进一步证实。我们的结果表明,这些化合物会干扰冠状病毒的感染性和复制过程。因此,这些新型化合物可能被证明是有效的广谱抗病毒抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b57/12406196/3096893a18f2/jm5c01602_0001.jpg

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