LETTER
Anti-BVDV Activity Evaluation of Naphthoimidazole Derivatives Compared with Parental Imidazoquinoline Compounds
Roberta Ibba*, 1, Sandra Piras1, Ilenia Delogu2, Roberta Loddo2, Antonio Carta1
Article Information
Identifiers and Pagination:
Year: 2020Volume: 14
First Page: 65
Last Page: 70
Publisher ID: TOMCJ-14-65
DOI: 10.2174/1874104502014010065
Article History:
Received Date: 6/5/2020Revision Received Date: 21/7/2020
Acceptance Date: 22/7/2020
Electronic publication date: 22/09/2020
Collection year: 2020
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.
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.