RESEARCH ARTICLE


Antiviral Activity of Benzotriazole Based Derivatives



Paola Corona1, Sandra Piras1, *, Roberta Ibba1, Federico Riu1, Gabriele Murineddu1, Giuseppina Sanna2, Silvia Madeddu2, Ilenia Delogu2, Roberta Loddo2, *, Antonio Carta1
1 Department of Chemistry and Pharmacy, University of Sassari, Via Muroni, 23/A, 07100 Sassari, Italy.
2 Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Italy.


© 2020 Corona 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 these authors at the Department of Chemistry and Pharmacy, University of Sassari, Via Muroni 23/A, 07100, Sassari, Italy; E-mail: piras@uniss.it and Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Italy; E-mail: rloddo@unica.it


Abstract

Background:

For the last thirty years, the benzotriazole scaffold has been the object of our group interest and we have already presented some results on the antiviral activity of our compounds.

Objective:

In this article, we conclude the exploration of N-(4-(R-2H-benzo[d][1,2,3]triazol-2-yl)phenyl)-4-R’-benzamides and 1-(4-(R-2H-benzo[d][1,2,3]triazol-2-yl)phenyl)-3-R’-ureas by synthesizing further modified derivatives, in order to have more elements for SARs evaluation.

Methods:

Here, we reported the synthesis and the antiviral screening results of 38 newly synthesized benzotriazole derivatives against a panel of DNA and RNA viruses. We also analyse SARs in comparing these compounds with previously published benzotriazole analogues, taking stock of the situation.

Results:

Among the newly presented derivatives, compounds 17 and 18 were the most active with EC50 6.9 and 5.5 µM, respectively against Coxsackievirus B5 (CV-B5) and 20.5 and 17.5 µM against Poliovirus (Sb-1).

Conclusion:

we can conclude that N-(4-(2H-benzo[d] [1 - 3] triazol-2-yl)phenyl-R-amide is a good chemical scaffold for the development of new antiviral molecules.

Keywords: Benzotriazole, Enteroviruses, CV-B5, Poliovirus, SARs, Antiviral.