Literature DB >> 24973816

Synthesis of new compounds with promising antiviral properties against group A and B Human Rhinoviruses.

Angela M Bernard1, Maria G Cabiddu2, Stefania De Montis1, Roberto Mura1, Raffaello Pompei3.   

Abstract

The human common cold, which is a benign disease caused by the Rhinoviruses, generally receives palliative symptomatic treatments, since no specific therapy against any of these viruses currently exists. In this work, some original synthetic compounds were produced and tested, in order to find non-toxic substances with an improved protection index (PI) for infected cells, as compared to reference drugs such as Pirodavir. We designed a series of novel molecules with a double oxygen in the central hydrocarbon chain and some modifications of the lateral methylisoxazole and propoxybenzoate moieties of lead compound 6602 (ethyl 4-{3-[2-(3-methyl-1,2-isoxazol-5-yl)ethoxy]propoxy}benzoate). It was found that most of these substances were actually less toxic than Pirodavir; in addition, the new molecule indicated as 8c was more than 30 times less toxic than Pirodavir, about twice as active on the group A strain of Rhinovirus HRV14, and even four times more effective on the group B strain HRV39, as compared to Pirodavir's PI.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antivirals; Cell receptors; Rhinoviruses

Mesh:

Substances:

Year:  2014        PMID: 24973816     DOI: 10.1016/j.bmc.2014.05.066

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  Exploration of the anti-enterovirus activity of a series of pleconaril/pirodavir-like compounds.

Authors:  Angela Bernard; Céline Lacroix; Maria G Cabiddu; Johan Neyts; Pieter Leyssen; Raffaello Pompei
Journal:  Antivir Chem Chemother       Date:  2015-06-11

2.  In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses.

Authors:  Céline Lacroix; Samuela Laconi; Fabrizio Angius; Antonio Coluccia; Romano Silvestri; Raffaello Pompei; Johan Neyts; Pieter Leyssen
Journal:  Virol J       Date:  2015-07-14       Impact factor: 4.099

Review 3.  Treatment of signs and symptoms of the common cold using EPs 7630 - results of a meta-analysis.

Authors:  Andreas Schapowal; Gustav Dobos; Holger Cramer; Kian Chung Ong; Martin Adler; Andrea Zimmermann; Juliette Brandes-Schramm; Walter Lehmacher
Journal:  Heliyon       Date:  2019-11-26

4.  Biological activity of 3-(2-benzoxazol-5-yl)alanine derivatives.

Authors:  Katarzyna Guzow; Ewa Mulkiewicz; Michał Obuchowski; Wiesław Wiczk
Journal:  Amino Acids       Date:  2021-07-08       Impact factor: 3.520

  4 in total

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