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Anti-BVDV Activity Evaluation of Naphthoimidazole Derivatives Compared with Parental Imidazoquinoline Compounds



Roberta Ibba*, 1, Sandra Piras1, Ilenia Delogu2, Roberta Loddo2, Antonio Carta1
1 Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23A, 07100 Sassari, Italy
2 Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042 Monserrato, Italy


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Creative Commons License
© 2020 Ibba et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: https://creativecommons.org/licenses/by/4.0/legalcode. This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the Department of Chemistry and Pharmacy, University of Sassari, Via Muroni 23/A, 07100 Sassari, Italy; E-mail: ribba@uniss.it.


Abstract

Background:

Pestivirus genus includes animal pathogens which are involved in economic impact for the livestock industry. Among others, Bovine Viral Diarrhoea Virus (BVDV) establish a persistent infection in cattle causing a long list of symptoms and a high mortality rate. In the last decades, we synthesised and reported a certain number of anti-BVDV compounds.

Methods:

In them, imidazoquinoline derivatives turned out as the most active. Their mechanism of actions has been deeply investigated, BVDV RNA-dependent RNA polymerase (RpRd) resulted as target and the way of binding was predicted in silico through three main H-bond interaction with the target.

The prediction could be confirmed by target or ligand mutation. The first approach has already been performed and published confirming the in silico prediction.

Results:

Here, we present how the ligand chemical modification affects the anti-BVDV activity. The designed compounds were synthesised and tested against BVDV as in silico assay negative control.

Conclusion:

The antiviral results confirmed the predicted mechanism of action, as the newly synthesised compounds resulted not active in the in vitro BVDV infection inhibition.

Keywords: BVDV, RdRp, Naphthoimidazoles, Antiviral activity, Pestivirus, Synthesis.