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Enhanced Remdesivir Analogues to Target SARS-CoV-2

We report the short synthesis of novel C-nucleoside Remdesivir analogues, their cytotoxicity and an in vitro evaluation against SARS-CoV-2 (CoV2). The described compounds are nucleoside analogues bearing a nitrogen heterocycle as purine analogues. The hybrid structures described herein are designed...

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Autores principales: Majima, Ryuichi, Edwards, Tiffany C., Dreis, Christine D., Geraghty, Robert J., Bonnac, Laurent F.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10052049/
https://www.ncbi.nlm.nih.gov/pubmed/36985586
http://dx.doi.org/10.3390/molecules28062616
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author Majima, Ryuichi
Edwards, Tiffany C.
Dreis, Christine D.
Geraghty, Robert J.
Bonnac, Laurent F.
author_facet Majima, Ryuichi
Edwards, Tiffany C.
Dreis, Christine D.
Geraghty, Robert J.
Bonnac, Laurent F.
author_sort Majima, Ryuichi
collection PubMed
description We report the short synthesis of novel C-nucleoside Remdesivir analogues, their cytotoxicity and an in vitro evaluation against SARS-CoV-2 (CoV2). The described compounds are nucleoside analogues bearing a nitrogen heterocycle as purine analogues. The hybrid structures described herein are designed to enhance the anti-CoV2 activity of Remdesivir. The compounds were evaluated for their cytotoxicity and their anti-CoV2 effect. We discuss the impact of combining both sugar and base modifications on the biological activities of these compounds, their lack of cytotoxicity and their antiviral efficacy.
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spelling pubmed-100520492023-03-30 Enhanced Remdesivir Analogues to Target SARS-CoV-2 Majima, Ryuichi Edwards, Tiffany C. Dreis, Christine D. Geraghty, Robert J. Bonnac, Laurent F. Molecules Communication We report the short synthesis of novel C-nucleoside Remdesivir analogues, their cytotoxicity and an in vitro evaluation against SARS-CoV-2 (CoV2). The described compounds are nucleoside analogues bearing a nitrogen heterocycle as purine analogues. The hybrid structures described herein are designed to enhance the anti-CoV2 activity of Remdesivir. The compounds were evaluated for their cytotoxicity and their anti-CoV2 effect. We discuss the impact of combining both sugar and base modifications on the biological activities of these compounds, their lack of cytotoxicity and their antiviral efficacy. MDPI 2023-03-13 /pmc/articles/PMC10052049/ /pubmed/36985586 http://dx.doi.org/10.3390/molecules28062616 Text en © 2023 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 Communication
Majima, Ryuichi
Edwards, Tiffany C.
Dreis, Christine D.
Geraghty, Robert J.
Bonnac, Laurent F.
Enhanced Remdesivir Analogues to Target SARS-CoV-2
title Enhanced Remdesivir Analogues to Target SARS-CoV-2
title_full Enhanced Remdesivir Analogues to Target SARS-CoV-2
title_fullStr Enhanced Remdesivir Analogues to Target SARS-CoV-2
title_full_unstemmed Enhanced Remdesivir Analogues to Target SARS-CoV-2
title_short Enhanced Remdesivir Analogues to Target SARS-CoV-2
title_sort enhanced remdesivir analogues to target sars-cov-2
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10052049/
https://www.ncbi.nlm.nih.gov/pubmed/36985586
http://dx.doi.org/10.3390/molecules28062616
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