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 |
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| Institution: | 1. Volgograd State Medical University, 400131 Volgograd, Russian Federation;2. N. F. Gamaleya National Research Center for Epidemiology and Microbiology, 123098 Moscow, Russian Federation;3. V. A. Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 119991 Moscow, Russian Federation;4. N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 119991 Moscow, Russian Federation;1. Hefei National Laboratory for Physical Sciences at the Microscale, University of Science and Technology of China, 230026 Hefei, China;2. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;1. Department of Materials Science, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;2. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;1. M. V. Lomonosov Institute of Fine Chemical Technologies, MIREA - Russian Technological University, 119454 Moscow, Russian Federation;2. Peptide Chemistry Research Center, K. N. Toosi University of Technology, P.O. Box 15875-4416, Tehran, Iran;3. Medical Biology Research Center, Kermanshah University of Medical Sciences, P. O. Box 67155-1616, Kermanshah, Iran;4. St. Petersburg State University, 199034 St. Petersburg, Russian Federation;5. Immanuel Kant Baltic Federal University, 236016 Kaliningrad, Russian Federation;1. N. S. Kurnakov Institute of General and Inorganic Chemistry, Russian Academy of Sciences, 119991 Moscow, Russian Federation;2. N. N. Semenov Research Center for Chemical Physics, Russian Academy of Sciences, 119991 Moscow, Russian Federation;1. Mental Health Research Institute, Tomsk National Research Medical Center, Russian Academy of Sciences, 634050 Tomsk, Russian Federation;2. Siberian State Medical University, 634050 Tomsk, Russian Federation;3. National Research Tomsk Polytechnic University, 634050 Tomsk, Russian Federation;4. Scientific Center for Mental Health, 115522 Moscow, Russian Federation;5. E. D. Goldberg Research Institute of Pharmacology and Regenerative Medicine, Tomsk National Research Medical Center, Russian Academy of Sciences, 634028 Tomsk, Russian Federation;1. M. M. Shemyakin–Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Russian Federation;2. National Medical Research Center for Obstetrics, Gynecology and Perinatology named after Academician V. I. Kulakov, 117997 Moscow, Russian Federation;3. N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 119991 Moscow, Russian Federation |
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| Abstract: | 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. |
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| Keywords: | uracil derivatives benzoic acid derivatives SARS-CoV-2 antiviral activity |
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