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Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives

The COVID-19 pandemic is ongoing as of mid-2022 and requires the development of new therapeutic drugs, because the existing clinically approved drugs are limited. In this work, seven derivatives of epoxybenzooxocinopyridine were synthesized and tested for the ability to inhibit the replication of th...

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Autores principales: Stalinskaya, Alena L., Martynenko, Nadezhda V., Shulgau, Zarina T., Shustov, Alexandr V., Keyer, Viktoriya V., Kulakov, Ivan V.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9230803/
https://www.ncbi.nlm.nih.gov/pubmed/35744830
http://dx.doi.org/10.3390/molecules27123701
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author Stalinskaya, Alena L.
Martynenko, Nadezhda V.
Shulgau, Zarina T.
Shustov, Alexandr V.
Keyer, Viktoriya V.
Kulakov, Ivan V.
author_facet Stalinskaya, Alena L.
Martynenko, Nadezhda V.
Shulgau, Zarina T.
Shustov, Alexandr V.
Keyer, Viktoriya V.
Kulakov, Ivan V.
author_sort Stalinskaya, Alena L.
collection PubMed
description The COVID-19 pandemic is ongoing as of mid-2022 and requires the development of new therapeutic drugs, because the existing clinically approved drugs are limited. In this work, seven derivatives of epoxybenzooxocinopyridine were synthesized and tested for the ability to inhibit the replication of the SARS-CoV-2 virus in cell cultures. Among the described compounds, six were not able to suppress the SARS-CoV-2 virus’ replication. One compound, which is a derivative of epoxybenzooxocinopyridine with an attached side group of 3,4-dihydroquinoxalin-2-one, demonstrated antiviral activity comparable to that of one pharmaceutical drug. The described compound is a prospective lead substance, because the half-maximal effective concentration is 2.23 μg/μL, which is within a pharmacologically achievable range.
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spelling pubmed-92308032022-06-25 Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives Stalinskaya, Alena L. Martynenko, Nadezhda V. Shulgau, Zarina T. Shustov, Alexandr V. Keyer, Viktoriya V. Kulakov, Ivan V. Molecules Article The COVID-19 pandemic is ongoing as of mid-2022 and requires the development of new therapeutic drugs, because the existing clinically approved drugs are limited. In this work, seven derivatives of epoxybenzooxocinopyridine were synthesized and tested for the ability to inhibit the replication of the SARS-CoV-2 virus in cell cultures. Among the described compounds, six were not able to suppress the SARS-CoV-2 virus’ replication. One compound, which is a derivative of epoxybenzooxocinopyridine with an attached side group of 3,4-dihydroquinoxalin-2-one, demonstrated antiviral activity comparable to that of one pharmaceutical drug. The described compound is a prospective lead substance, because the half-maximal effective concentration is 2.23 μg/μL, which is within a pharmacologically achievable range. MDPI 2022-06-09 /pmc/articles/PMC9230803/ /pubmed/35744830 http://dx.doi.org/10.3390/molecules27123701 Text en © 2022 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
Stalinskaya, Alena L.
Martynenko, Nadezhda V.
Shulgau, Zarina T.
Shustov, Alexandr V.
Keyer, Viktoriya V.
Kulakov, Ivan V.
Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives
title Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives
title_full Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives
title_fullStr Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives
title_full_unstemmed Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives
title_short Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives
title_sort synthesis and antiviral properties against sars-cov-2 of epoxybenzooxocino[4,3-b]pyridine derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9230803/
https://www.ncbi.nlm.nih.gov/pubmed/35744830
http://dx.doi.org/10.3390/molecules27123701
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