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ЖУРНАЛЫ // Mendeleev Communications // Архив

Mendeleev Commun., 2023, том 33, выпуск 4, страницы 537–538 (Mi mendc452)

Communications

New N1-(4-aryloxybenzyl)uracils containing N3-positioned 4-(trimethyleneoxy)benzoic acid moiety, and study of their antiviral activity against SARS-CoV-2 and influenza virus

M. S. Novikova, M. P. Paramonovaa, I. M. Kirillovb, O. A. Smirnovac, A. L. Khandazhinskayac, A. O. Chizhovd, S. N. Kochetkovc, A. V. Ivanovc, I. F. Fedyakinab

a Volgograd State Medical University, Volgograd, Russian Federation
b N.F. Gamaleya National Research Center for Epidemiology and Microbiology, Moscow, Russian Federation
c V.A. Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, Russian Federation
d N.D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, Russian Federation


Аннотация: New title uracil derivatives, 4-{3-[2,6-dioxo-3-(4-aryl-oxybenzyl)-3,6-dihydropyrimidin-1(2H)-yl]propoxy}benzoic acids and their butoxy homologues, were obtained in three steps using 2,4-bis(trimethylsilyloxy)pyrimidine, 4-aryloxy-benzyl bromides and methyl 4-(ω-bromoalkoxy)benzoates as the key reactants. The compounds were studied as inhibitors of H1N1 influenza virus and SARS-CoV-2 R replication in MDCK and Vero E6 cell cultures, respectively, which revealed that the tested compounds had high levels of anti-SARS-CoV-2 activity.

Ключевые слова: uracil derivatives, benzoic acid derivatives, SARS-CoV-2, antiviral activity, N-alkylation.

Язык публикации: английский

DOI: 10.1016/j.mencom.2023.06.031



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