New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity
Pyrimidine nucleoside analogues are widely used to treat infections caused by the human immunodeficiency virus (HIV) and DNA viruses from the herpes family. It has been shown that 5-substituted uracil derivatives can inhibit HIV-1, herpes family viruses, mycobacteria and other pathogens through vari...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/9/2866 |
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| author | Vasily A. Kezin Elena S. Matyugina Mikhail S. Novikov Alexander O. Chizhov Robert Snoeck Graciela Andrei Sergei N. Kochetkov Anastasia L. Khandazhinskaya |
| author_facet | Vasily A. Kezin Elena S. Matyugina Mikhail S. Novikov Alexander O. Chizhov Robert Snoeck Graciela Andrei Sergei N. Kochetkov Anastasia L. Khandazhinskaya |
| author_sort | Vasily A. Kezin |
| collection | DOAJ |
| description | Pyrimidine nucleoside analogues are widely used to treat infections caused by the human immunodeficiency virus (HIV) and DNA viruses from the herpes family. It has been shown that 5-substituted uracil derivatives can inhibit HIV-1, herpes family viruses, mycobacteria and other pathogens through various mechanisms. Among the 5-substituted pyrimidine nucleosides, there are not only the classical nucleoside inhibitors of the herpes family viruses, 2′-deoxy-5-iodocytidine and 5-bromovinyl-2′-deoxyuridine, but also derivatives of 1-(benzyl)-5-(phenylamino)uracil, which proved to be non-nucleoside inhibitors of HIV-1 and EBV. It made this modification of nucleoside analogues very promising in connection with the emergence of new viruses and the crisis of drug resistance when the task of creating effective antiviral agents of new types that act on other targets or exhibit activity by other mechanisms is very urgent. In this paper, we present the design, synthesis and primary screening of the biological activity of new nucleoside analogues, namely, 5′-norcarbocyclic derivatives of substituted 5-arylamino- and 5-aryloxyuracils, against RNA viruses. |
| first_indexed | 2024-03-10T03:53:59Z |
| format | Article |
| id | doaj.art-ba7d97f4d9c742ed9afcdcc355080063 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T03:53:59Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-ba7d97f4d9c742ed9afcdcc3550800632023-11-23T08:50:49ZengMDPI AGMolecules1420-30492022-04-01279286610.3390/molecules27092866New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological ActivityVasily A. Kezin0Elena S. Matyugina1Mikhail S. Novikov2Alexander O. Chizhov3Robert Snoeck4Graciela Andrei5Sergei N. Kochetkov6Anastasia L. Khandazhinskaya7Engelhardt Institute of Molecular Biology, Russian Academy of Science, 119991 Moscow, RussiaEngelhardt Institute of Molecular Biology, Russian Academy of Science, 119991 Moscow, RussiaDepartment of Pharmaceutical & Toxicological Chemistry, Volgograd State Medical University, 400131 Volgograd, RussiaN.D. Zelinsky Institute of Organic Chemistry, Russian Academy of Science, Leninski pr. 47, 119991 Moscow, RussiaRega Institute for Medical Research, KU Leuven, B-3000 Leuven, BelgiumRega Institute for Medical Research, KU Leuven, B-3000 Leuven, BelgiumEngelhardt Institute of Molecular Biology, Russian Academy of Science, 119991 Moscow, RussiaEngelhardt Institute of Molecular Biology, Russian Academy of Science, 119991 Moscow, RussiaPyrimidine nucleoside analogues are widely used to treat infections caused by the human immunodeficiency virus (HIV) and DNA viruses from the herpes family. It has been shown that 5-substituted uracil derivatives can inhibit HIV-1, herpes family viruses, mycobacteria and other pathogens through various mechanisms. Among the 5-substituted pyrimidine nucleosides, there are not only the classical nucleoside inhibitors of the herpes family viruses, 2′-deoxy-5-iodocytidine and 5-bromovinyl-2′-deoxyuridine, but also derivatives of 1-(benzyl)-5-(phenylamino)uracil, which proved to be non-nucleoside inhibitors of HIV-1 and EBV. It made this modification of nucleoside analogues very promising in connection with the emergence of new viruses and the crisis of drug resistance when the task of creating effective antiviral agents of new types that act on other targets or exhibit activity by other mechanisms is very urgent. In this paper, we present the design, synthesis and primary screening of the biological activity of new nucleoside analogues, namely, 5′-norcarbocyclic derivatives of substituted 5-arylamino- and 5-aryloxyuracils, against RNA viruses.https://www.mdpi.com/1420-3049/27/9/28665′-norcarbocyclic nucleoside analogueschemical synthesisRNA viruses |
| spellingShingle | Vasily A. Kezin Elena S. Matyugina Mikhail S. Novikov Alexander O. Chizhov Robert Snoeck Graciela Andrei Sergei N. Kochetkov Anastasia L. Khandazhinskaya New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity Molecules 5′-norcarbocyclic nucleoside analogues chemical synthesis RNA viruses |
| title | New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity |
| title_full | New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity |
| title_fullStr | New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity |
| title_full_unstemmed | New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity |
| title_short | New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity |
| title_sort | new derivatives of 5 substituted uracils potential agents with a wide spectrum of biological activity |
| topic | 5′-norcarbocyclic nucleoside analogues chemical synthesis RNA viruses |
| url | https://www.mdpi.com/1420-3049/27/9/2866 |
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