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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...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2022
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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. |
format | Online Article Text |
id | pubmed-9230803 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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