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About:
Dichloro-Phenyl-Benzotriazoles: A New Selective Class of Human Respiratory Syncytial Virus Entry Inhibitors
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An Entity of Type :
schema:ScholarlyArticle
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wasabi.inria.fr
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Type:
Academic Article
research paper
schema:ScholarlyArticle
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type
Academic Article
research paper
schema:ScholarlyArticle
isDefinedBy
Covid-on-the-Web dataset
has title
Dichloro-Phenyl-Benzotriazoles: A New Selective Class of Human Respiratory Syncytial Virus Entry Inhibitors
Creator
Loddo, Roberta
Madeddu, Silvia
Sanna, Giuseppina
Aulic, Suzana
Caria, Paola
Carta, Antonio
Corona, Paola
Fermeglia, Maurizio
Ibba, Roberta
Laurini, Erik
Piras, Sandra
Pricl, Sabrina
Désaubry, Laurent
Costi, Maria
Sadiq, Abdul
Source
PMC
abstract
Human Respiratory Syncytial Virus (RSV) is the primary cause of bronchopneumonia in infants and children worldwide. Clinical studies have shown that early treatments of RSV patients with ribavirin improve prognosis, even if the use of this drug is limited due to myelosuppression and toxicity effects. Furthermore, effective vaccines to prevent RSV infection are currently unavailable. Thus, the development of highly effective and specific antiviral drugs for pre-exposure prophylaxis and/or treatment of RSV infections is a compelling need. In the quest of new RSV inhibitors, in this work we evaluated the antiviral activity of a series of variously substituted 5,6-dichloro-1-phenyl-1(2)H-benzo[d][1,2,3]triazole derivatives in cell-based assays. Several 1- and 2-phenyl-benzotriazoles resulted fairly potent (μM concentrations) inhibitors of RSV infection in plaque reduction assays, accompanied by low cytotoxicity in human highly dividing T lymphoid-derived cells and primary cell lines. Contextually, no inhibitory effects were observed against other RNA or DNA viruses assayed, suggesting specific activity against RSV. Further results revealed that the lead compound 10d was active during the early phase of the RSV infection cycle. To understand whether 10d interfered with virus attachment to target cells or virus-cell fusion events, inhibitory activity tests against the RSV mutant strain B1 cp-52—expressing only the F envelope glycoprotein—and a plasmid-based reporter assay that quantifies the bioactivity of viral entry were also performed. The overall biological results, in conjunction with in silico modeling studies, supported the conclusion that the RSV fusion process could be the target of this new series of compounds.
has issue date
2019-04-16
(
xsd:dateTime
)
bibo:doi
10.3389/fchem.2019.00247
bibo:pmid
31041309
has license
cc-by
sha1sum (hex)
48215f45ce10b06c8f96b087cf1d72de2b40662a
schema:url
https://doi.org/10.3389/fchem.2019.00247
resource representing a document's title
Dichloro-Phenyl-Benzotriazoles: A New Selective Class of Human Respiratory Syncytial Virus Entry Inhibitors
has PubMed Central identifier
PMC6476926
has PubMed identifier
31041309
schema:publication
Front Chem
resource representing a document's body
covid:48215f45ce10b06c8f96b087cf1d72de2b40662a#body_text
is
schema:about
of
named entity 'DERIVED'
named entity 'LOW'
named entity 'CELLS'
named entity 'PLAQUE'
named entity 'DUE TO'
named entity '282'
named entity 'ENVELOPE GLYCOPROTEIN'
named entity 'RNA'
named entity 'VIRUS ATTACHMENT'
named entity 'IS A'
named entity 'UNDERSTAND'
named entity 'HUMAN RESPIRATORY SYNCYTIAL VIRUS'
named entity 'SUPPORTED'
named entity 'ANTIVIRAL ACTIVITY'
named entity 'VIRAL ENTRY'
named entity 'RSV'
named entity 'INHIBITORY ACTIVITY'
named entity 'BRONCHOPNEUMONIA'
named entity 'RSV INFECTIONS'
named entity 'REDUCTION'
named entity 'PERFORMED'
named entity 'PRIMARY'
named entity 'BASED'
named entity 'CONCLUSION'
named entity 'DEVELOPMENT'
named entity '2C6'
named entity 'LYMPHOID'
named entity 'STUDIES'
named entity 'PHENYL'
named entity 'fusion'
named entity 'virus'
named entity 'development'
named entity 'Selective'
named entity 'PHENYL'
named entity 'SERIES'
named entity 'LEAD COMPOUND'
named entity 'IN SILICO'
named entity 'BENZOTRIAZOLES'
named entity 'PRE-EXPOSURE PROPHYLAXIS'
named entity 'HUMAN'
named entity 'PROCESS'
named entity 'PROGNOSIS'
named entity 'PATIENTS'
named entity 'RESULTS'
named entity 'FUSION'
named entity 'MYELOSUPPRESSION'
named entity 'TREATMENTS'
named entity 'CELL FUSION'
named entity '10D'
named entity 'WORLDWIDE'
named entity 'OVERALL'
named entity 'TO PREVENT'
named entity 'TARGET CELLS'
named entity 'OBSERVED'
named entity 'BIOLOGICAL'
named entity 'COULD BE'
named entity 'SPECIFIC'
named entity '5B1'
named entity 'TREATMENT'
named entity 'WORK'
named entity 'EARLY'
named entity 'UNAVAILABLE'
named entity 'INFANTS'
named entity 'TESTS'
covid:arg/48215f45ce10b06c8f96b087cf1d72de2b40662a
named entity 'CLASS'
named entity 'BENZOTRIAZOLES'
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