LETTER

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

The Open Medicinal Chemistry Journal 22 Sept 2020 LETTER DOI: 10.2174/1874104502014010065

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.
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