Title: Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor
Authors: 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 # ×
Issue Date: Nov-2016
Series Title: European Journal of Medicinal Chemistry vol:124 pages:773-781
Article number: S0223-5234(16)30740-1
Abstract: 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.
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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