Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues

Despite the fact that COVID-19 vaccines are already available on the market, there have not been any effective FDA-approved drugs to treat this disease. There are several already known drugs that through drug repositioning have shown an inhibitory activity against SARS-CoV-2 RNA-dependent RNA polyme...

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Autores principales: Daikopoulou, Vasiliki, Apostolou, Panagiotis, Mourati, Sofia, Vlachou, Ioanna, Gougousi, Maria, Papasotiriou, Ioannis
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8201013/
https://www.ncbi.nlm.nih.gov/pubmed/34200204
http://dx.doi.org/10.3390/molecules26113461
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author Daikopoulou, Vasiliki
Apostolou, Panagiotis
Mourati, Sofia
Vlachou, Ioanna
Gougousi, Maria
Papasotiriou, Ioannis
author_facet Daikopoulou, Vasiliki
Apostolou, Panagiotis
Mourati, Sofia
Vlachou, Ioanna
Gougousi, Maria
Papasotiriou, Ioannis
author_sort Daikopoulou, Vasiliki
collection PubMed
description Despite the fact that COVID-19 vaccines are already available on the market, there have not been any effective FDA-approved drugs to treat this disease. There are several already known drugs that through drug repositioning have shown an inhibitory activity against SARS-CoV-2 RNA-dependent RNA polymerase. These drugs are included in the family of nucleoside analogues. In our efforts, we synthesized a group of new nucleoside analogues, which are modified at the sugar moiety that is replaced by a quinazoline entity. Different nucleobase derivatives are used in order to increase the inhibition. Five new nucleoside analogues were evaluated with in vitro assays for targeting polymerase of SARS-CoV-2.
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spelling pubmed-82010132021-06-15 Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues Daikopoulou, Vasiliki Apostolou, Panagiotis Mourati, Sofia Vlachou, Ioanna Gougousi, Maria Papasotiriou, Ioannis Molecules Article Despite the fact that COVID-19 vaccines are already available on the market, there have not been any effective FDA-approved drugs to treat this disease. There are several already known drugs that through drug repositioning have shown an inhibitory activity against SARS-CoV-2 RNA-dependent RNA polymerase. These drugs are included in the family of nucleoside analogues. In our efforts, we synthesized a group of new nucleoside analogues, which are modified at the sugar moiety that is replaced by a quinazoline entity. Different nucleobase derivatives are used in order to increase the inhibition. Five new nucleoside analogues were evaluated with in vitro assays for targeting polymerase of SARS-CoV-2. MDPI 2021-06-07 /pmc/articles/PMC8201013/ /pubmed/34200204 http://dx.doi.org/10.3390/molecules26113461 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Daikopoulou, Vasiliki
Apostolou, Panagiotis
Mourati, Sofia
Vlachou, Ioanna
Gougousi, Maria
Papasotiriou, Ioannis
Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues
title Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues
title_full Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues
title_fullStr Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues
title_full_unstemmed Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues
title_short Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues
title_sort targeting sars-cov-2 polymerase with new nucleoside analogues
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8201013/
https://www.ncbi.nlm.nih.gov/pubmed/34200204
http://dx.doi.org/10.3390/molecules26113461
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