Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs

The COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is continuing to spread around the world. GS-441524 is the parent nucleoside of remdesivir which is the first drug approved for the treatment of COVID-19, and demonstrates strong activity against SARS-Cov-2 in vitro...

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Autores principales: Zheng, Wei, Hu, Tianwen, Zhang, Yumin, Wei, Daibao, Xie, Yuanchao, Shen, Jingshan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9270844/
https://www.ncbi.nlm.nih.gov/pubmed/35844292
http://dx.doi.org/10.1016/j.tetlet.2022.154012
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author Zheng, Wei
Hu, Tianwen
Zhang, Yumin
Wei, Daibao
Xie, Yuanchao
Shen, Jingshan
author_facet Zheng, Wei
Hu, Tianwen
Zhang, Yumin
Wei, Daibao
Xie, Yuanchao
Shen, Jingshan
author_sort Zheng, Wei
collection PubMed
description The COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is continuing to spread around the world. GS-441524 is the parent nucleoside of remdesivir which is the first drug approved for the treatment of COVID-19, and demonstrates strong activity against SARS-Cov-2 in vitro and in vivo. Herein, we reported the synthesis of a series of deuterated GS-441524 analogs, which had deuterium atoms up to five at the ribose and the nucleobase moieties. Compared to GS-441524, all the deuterated compounds showed similar inhibitory activities against SARS-CoV-2 in vitro.
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spelling pubmed-92708442022-07-11 Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs Zheng, Wei Hu, Tianwen Zhang, Yumin Wei, Daibao Xie, Yuanchao Shen, Jingshan Tetrahedron Lett Article The COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is continuing to spread around the world. GS-441524 is the parent nucleoside of remdesivir which is the first drug approved for the treatment of COVID-19, and demonstrates strong activity against SARS-Cov-2 in vitro and in vivo. Herein, we reported the synthesis of a series of deuterated GS-441524 analogs, which had deuterium atoms up to five at the ribose and the nucleobase moieties. Compared to GS-441524, all the deuterated compounds showed similar inhibitory activities against SARS-CoV-2 in vitro. Elsevier Ltd. 2022-08-17 2022-07-09 /pmc/articles/PMC9270844/ /pubmed/35844292 http://dx.doi.org/10.1016/j.tetlet.2022.154012 Text en © 2022 Elsevier Ltd. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Zheng, Wei
Hu, Tianwen
Zhang, Yumin
Wei, Daibao
Xie, Yuanchao
Shen, Jingshan
Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
title Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
title_full Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
title_fullStr Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
title_full_unstemmed Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
title_short Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
title_sort synthesis and anti-sars-cov-2 activity of deuterated gs-441524 analogs
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9270844/
https://www.ncbi.nlm.nih.gov/pubmed/35844292
http://dx.doi.org/10.1016/j.tetlet.2022.154012
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