Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity

A series of 2-amino-5-bromo-4(3H)-pyrimidinone derivatives bearing different substituents at the C-6 position were synthesized using a highly regioselective lithiation–substitution protocol, and the effect of structural variation at the C-6 position on their antiviral activity in cell culture was ev...

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Detalles Bibliográficos
Autores principales: Singh, Kamaljit, Singh, Kawaljit, Balzarini, Jan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2013
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127258/
https://www.ncbi.nlm.nih.gov/pubmed/23911856
http://dx.doi.org/10.1016/j.ejmech.2013.06.036
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author Singh, Kamaljit
Singh, Kawaljit
Balzarini, Jan
author_facet Singh, Kamaljit
Singh, Kawaljit
Balzarini, Jan
author_sort Singh, Kamaljit
collection PubMed
description A series of 2-amino-5-bromo-4(3H)-pyrimidinone derivatives bearing different substituents at the C-6 position were synthesized using a highly regioselective lithiation–substitution protocol, and the effect of structural variation at the C-6 position on their antiviral activity in cell culture was evaluated. Although some of the derivatives were found to be active against various virus strains, they were effective only close to their toxicity threshold.
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spelling pubmed-71272582020-04-08 Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity Singh, Kamaljit Singh, Kawaljit Balzarini, Jan Eur J Med Chem Original Article A series of 2-amino-5-bromo-4(3H)-pyrimidinone derivatives bearing different substituents at the C-6 position were synthesized using a highly regioselective lithiation–substitution protocol, and the effect of structural variation at the C-6 position on their antiviral activity in cell culture was evaluated. Although some of the derivatives were found to be active against various virus strains, they were effective only close to their toxicity threshold. Elsevier Masson SAS. 2013-09 2013-07-05 /pmc/articles/PMC7127258/ /pubmed/23911856 http://dx.doi.org/10.1016/j.ejmech.2013.06.036 Text en Copyright © 2013 Elsevier Masson SAS. 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 Original Article
Singh, Kamaljit
Singh, Kawaljit
Balzarini, Jan
Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity
title Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity
title_full Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity
title_fullStr Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity
title_full_unstemmed Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity
title_short Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity
title_sort regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3h)-pyrimidinones and evaluation of their antiviral activity
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127258/
https://www.ncbi.nlm.nih.gov/pubmed/23911856
http://dx.doi.org/10.1016/j.ejmech.2013.06.036
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