About: Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor

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About: Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor
Creator	Balzarini, Jan Andrei, Graciela Snoeck, Robert Bertamino, Alessia Campiglia, Pietro Ciaglia, Tania Musella, Simona Novellino, Ettore Ostacolo, Carmine Sala, Marina Spensiero, Antonia Di Sarno, Veronica Gomez-Monterrey, Isabel Scala, Maria
Source	Elsevier; Medline; PMC
abstract	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.
has issue date	2016-11-29(xsd:dateTime)
bibo:doi	10.1016/j.ejmech.2016.09.014
bibo:pmid	27639368
has license	els-covid
sha1sum (hex)	520dbf78a2d1b45e3c6d949158dae1c5c0f536f7
schema:url	https://doi.org/10.1016/j.ejmech.2016.09.014
resource representing a document's title	Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor
has PubMed Central identifier	PMC7115581
has PubMed identifier	27639368
schema:publication	European Journal of Medicinal Chemistry
resource representing a document's body	covid:520dbf78a2d1b45e3c6d949158dae1c5c0f536f7#body_text
is schema:about of	named entity 'DERIVATIVE' named entity 'tested' named entity 'varicella zoster virus' named entity 'reactions' named entity 'coupled' named entity 'SAR' named entity 'Modifications' named entity 'VARICELLA ZOSTER VIRUS' named entity 'INHIBITOR' named entity 'AMINATIONS' named entity 'VARIETY' named entity 'VARICELLA ZOSTER VIRUS' named entity 'TEMPLATE' named entity 'COMPETENT' covid:arg/520dbf78a2d1b45e3c6d949158dae1c5c0f536f7 named entity 'ANTIVIRAL ACTIVITY' named entity 'DERIVATIVE' named entity 'FINAL' named entity 'VZV' named entity 'ACTIVITY' named entity 'REPLICATION' named entity 'INDOLE' named entity 'STRAINS' named entity '17A' named entity 'NOVEL' named entity 'BASED' named entity 'BEING' named entity 'REDUCTIVE' named entity 'LED' named entity 'STUDY' named entity 'SELECTIVE' named entity 'REPORT' named entity 'DISPLACEMENT' named entity 'AMINO GROUP' named entity 'NEW' named entity 'MECHANISM' named entity 'MOIETY' named entity 'NON-' named entity 'COUPLED' named entity 'BIPHENYL' named entity 'HUMAN' named entity 'DERIVED' named entity 'TESTED' named entity 'THYMIDINE KINASE' named entity 'ANTIVIRALS' named entity 'SELECTIVE' named entity 'NUCLEUS' named entity 'ETHYL' named entity 'IDENTIFICATION' named entity 'CRAFTS' named entity 'COMPOUND' named entity 'INACTIVE' named entity 'FOUND' named entity 'STRUCTURE-ACTIVITY RELATIONSHIP' named entity 'PRESENCE OF' named entity 'NUCLEOSIDE' named entity 'DNA' named entity 'PREREQUISITE' named entity 'HAVE' named entity 'IN VITRO' named entity 'POINTING' named entity 'TRYPTAMINE' named entity 'RNA VIRUSES' named entity 'ACETYLATION' named entity 'REACTIONS' named entity 'SYNTHESIS' named entity 'INHIBITORY ACTIVITY' named entity 'INDOL'

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