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Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses

Picornaviridae represent a very large family of small RNA viruses, some of which are the cause of important human and animal diseases. Since no specific therapy against any of these viruses currently exists, palliative symptomatic treatments are employed. The early steps of the picornavirus replicat...

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Autores principales: Laconi, Samuela, Madeddu, Maria A., Pompei, Raffaello
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6263271/
https://www.ncbi.nlm.nih.gov/pubmed/21522081
http://dx.doi.org/10.3390/molecules16053479
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author Laconi, Samuela
Madeddu, Maria A.
Pompei, Raffaello
author_facet Laconi, Samuela
Madeddu, Maria A.
Pompei, Raffaello
author_sort Laconi, Samuela
collection PubMed
description Picornaviridae represent a very large family of small RNA viruses, some of which are the cause of important human and animal diseases. Since no specific therapy against any of these viruses currently exists, palliative symptomatic treatments are employed. The early steps of the picornavirus replicative cycle seem to be privileged targets for some antiviral compounds like disoxaril and pirodavir. Pirodavir’s main weakness is its cytotoxicity on cell cultures at relatively low doses. In this work some original synthetic compounds were tested, in order to find less toxic compounds with an improved protection index (PI) on infected cells. Using an amino group to substitute the oxygen atom in the central chain, such as that in the control molecule pirodavir, resulted in decreased activity against Rhinoviruses and Polioviruses. The presence of an -ethoxy-propoxy- group in the central chain (as in compound I-6602) resulted in decreased cell toxicity and in improved anti-Rhinovirus activity. This compound actually showed a PI >700 on HRV14, while pirodavir had a PI of 250. These results demonstrate that modification of pirodavir’s central hydrocarbon chain can lead to the production of novel derivatives with low cytotoxicity and improved PI against some strains of Rhinoviruses.
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spelling pubmed-62632712018-12-10 Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses Laconi, Samuela Madeddu, Maria A. Pompei, Raffaello Molecules Article Picornaviridae represent a very large family of small RNA viruses, some of which are the cause of important human and animal diseases. Since no specific therapy against any of these viruses currently exists, palliative symptomatic treatments are employed. The early steps of the picornavirus replicative cycle seem to be privileged targets for some antiviral compounds like disoxaril and pirodavir. Pirodavir’s main weakness is its cytotoxicity on cell cultures at relatively low doses. In this work some original synthetic compounds were tested, in order to find less toxic compounds with an improved protection index (PI) on infected cells. Using an amino group to substitute the oxygen atom in the central chain, such as that in the control molecule pirodavir, resulted in decreased activity against Rhinoviruses and Polioviruses. The presence of an -ethoxy-propoxy- group in the central chain (as in compound I-6602) resulted in decreased cell toxicity and in improved anti-Rhinovirus activity. This compound actually showed a PI >700 on HRV14, while pirodavir had a PI of 250. These results demonstrate that modification of pirodavir’s central hydrocarbon chain can lead to the production of novel derivatives with low cytotoxicity and improved PI against some strains of Rhinoviruses. MDPI 2011-04-26 /pmc/articles/PMC6263271/ /pubmed/21522081 http://dx.doi.org/10.3390/molecules16053479 Text en © 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Laconi, Samuela
Madeddu, Maria A.
Pompei, Raffaello
Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses
title Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses
title_full Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses
title_fullStr Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses
title_full_unstemmed Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses
title_short Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses
title_sort study of the biological activity of novel synthetic compounds with antiviral properties against human rhinoviruses
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6263271/
https://www.ncbi.nlm.nih.gov/pubmed/21522081
http://dx.doi.org/10.3390/molecules16053479
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