2. Academic Validation
  3. Quinoxaline derivatives as new inhibitors of coxsackievirus B5

Quinoxaline derivatives as new inhibitors of coxsackievirus B5

  • Eur J Med Chem. 2018 Feb 10:145:559-569. doi: 10.1016/j.ejmech.2017.12.083.
Antonio Carta 1,  Giuseppina Sanna 2,  Irene Briguglio 3,  Silvia Madeddu 4,  Gabriella Vitale 3,  Sandra Piras 3,  Paola Corona 3,  Alessandra Tiziana Peana 3,  Erik Laurini 5,  Maurizio Fermeglia 5,  Sabrina Pricl 5,  Alessandra Serra 4,  Elisa Carta 4,  Roberta Loddo 4,  Gabriele Giliberti 4
Affiliations

Affiliations

  • 1 Department of Chemistry and Pharmacy, University of Sassari, Via Muroni 23, 07100 Sassari, Italy. Electronic address: acarta@uniss.it.
  • 2 Department of Biomedical Sciences, University of Cagliari, Cittadella Universitaria, 09042 Monserrato, Cagliari, Italy. Electronic address: g.sanna@unica.it.
  • 3 Department of Chemistry and Pharmacy, University of Sassari, Via Muroni 23, 07100 Sassari, Italy.
  • 4 Department of Biomedical Sciences, University of Cagliari, Cittadella Universitaria, 09042 Monserrato, Cagliari, Italy.
  • 5 Molecular Simulation Engineering (MOSE) Laboratory, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy.
PMID: 29339251 DOI: 10.1016/j.ejmech.2017.12.083
Abstract

Enteroviruses are among the most common and important human pathogens for which there are no specific Antiviral agents approved by the US Food and Drug Administration so far. Particularly, coxsackievirus infections have a worldwide distribution and can cause many important diseases. We here report the synthesis of new 14 quinoxaline derivatives and the evaluation of their cytotoxicity and Antiviral activity against representatives of ssRNA, dsRNA and dsDNA viruses. Promisingly, three compounds showed a very potent and selective Antiviral activity against coxsackievirus B5, with EC50 in the sub-micromolar range (0.3-0.06 μM). A combination of experimental techniques (i.e. virucidal activity, time of drug addition and adsorption assays) and in silico modeling studies were further performed, aiming to understand the mode of action of the most active, selective and not cytotoxic compound, the ethyl 4-[(2,3-dimethoxyquinoxalin-6-yl)methylthio]benzoate (6).

Keywords

Antiviral activity; Enteroviruses; Viral protein VP1; in silico modeling.

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