European journal of medicinal chemistry · 2016
Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor.
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Musella Simona, di Sarno Veronica, Ciaglia Tania, Sala Marina, Spensiero Antonia, Scala Maria Carmina, Ostacolo Carmine, Andrei Graciela, Balzarini Jan, Snoeck Robert, Novellino Ettore, Campiglia Pietro, Bertamino Alessia, Gomez-Monterrey Isabel M
Аннотация
We report the synthesis and antiviral activity of a new family of non-nucleoside antivirals, derived from the indole nucleus. Modifications of this template through Mannich and Friedel-Crafts reactions, coupled with nucleophilic displacement and reductive aminations led to 23 final derivatives, which were pharmacologically tested. Tryptamine derivative 17a was found to have a selective inhibitory activity against human varicella zoster virus (VZV) replication in vitro, being inactive against a variety of other DNA and RNA viruses. A structure-activity relationship (SAR) study showed that the presence of a biphenyl ethyl moiety and the acetylation at the amino group of tryptamine are a prerequisite for anti-VZV activity. The novel compound shows the same activity against thymidine kinase (TK)-competent (TK+) and TK-deficient (TK-) VZV strains, pointing to a novel mechanism of antiviral action.