Carta, Antonio and Sanna, Giuseppina and Briguglio, Irene and Madeddu, Silvia and Vitale, Gabriella and Piras, Sandra and Corona, Paola and Peana, Alessandra Tiziana and Laurini, Erik and Fermeglia, Maurizio and Pricl, Sabrina and Serra, Alessandra and Carta, Elisa and Loddo, Roberta and Gilberti, Gabriele (2018) Quinoxaline derivatives as new inhibitors of coxsackievirus B5. European Journal of Medicinal Chemistry, Vol. 145 , p. 559-569. ISSN 0223-5234. Article.
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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).
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