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Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture.

Identifieur interne : 002389 ( PubMed/Corpus ); précédent : 002388; suivant : 002390

Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture.

Auteurs : Jan Balzarini ; Els Keyaerts ; Leen Vijgen ; Frank Vandermeer ; Miguel Stevens ; Erik De Clercq ; Herman Egberink ; Marc Van Ranst

Source :

RBID : pubmed:16387746

English descriptors

Abstract

Evaluation of a wide variety of pyridine N-oxide derivatives on their inhibitory activity against feline coronavirus (FIPV strain) and human SARS-CoV (Frankfurt strain-1) in cell culture.

DOI: 10.1093/jac/dki481
PubMed: 16387746

Links to Exploration step

pubmed:16387746

Le document en format XML

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<title xml:lang="en">Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture.</title>
<author>
<name sortKey="Balzarini, Jan" sort="Balzarini, Jan" uniqKey="Balzarini J" first="Jan" last="Balzarini">Jan Balzarini</name>
<affiliation>
<nlm:affiliation>Rega Institute for Medical Research, K.U. Leuven, Leuven, Belgium. jan.balzarini@rega.kuleuven.ac.be</nlm:affiliation>
</affiliation>
</author>
<author>
<name sortKey="Keyaerts, Els" sort="Keyaerts, Els" uniqKey="Keyaerts E" first="Els" last="Keyaerts">Els Keyaerts</name>
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<author>
<name sortKey="Vijgen, Leen" sort="Vijgen, Leen" uniqKey="Vijgen L" first="Leen" last="Vijgen">Leen Vijgen</name>
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<name sortKey="Vandermeer, Frank" sort="Vandermeer, Frank" uniqKey="Vandermeer F" first="Frank" last="Vandermeer">Frank Vandermeer</name>
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<name sortKey="Stevens, Miguel" sort="Stevens, Miguel" uniqKey="Stevens M" first="Miguel" last="Stevens">Miguel Stevens</name>
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<name sortKey="De Clercq, Erik" sort="De Clercq, Erik" uniqKey="De Clercq E" first="Erik" last="De Clercq">Erik De Clercq</name>
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<name sortKey="Egberink, Herman" sort="Egberink, Herman" uniqKey="Egberink H" first="Herman" last="Egberink">Herman Egberink</name>
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<name sortKey="Van Ranst, Marc" sort="Van Ranst, Marc" uniqKey="Van Ranst M" first="Marc" last="Van Ranst">Marc Van Ranst</name>
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<name sortKey="Vandermeer, Frank" sort="Vandermeer, Frank" uniqKey="Vandermeer F" first="Frank" last="Vandermeer">Frank Vandermeer</name>
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<name sortKey="Stevens, Miguel" sort="Stevens, Miguel" uniqKey="Stevens M" first="Miguel" last="Stevens">Miguel Stevens</name>
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<title level="j">The Journal of antimicrobial chemotherapy</title>
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<term>Animals</term>
<term>Antiviral Agents (chemistry)</term>
<term>Antiviral Agents (pharmacology)</term>
<term>Cats</term>
<term>Cells, Cultured</term>
<term>Coronavirus, Feline (drug effects)</term>
<term>Humans</term>
<term>Molecular Structure</term>
<term>Pyridines (chemistry)</term>
<term>Pyridines (pharmacology)</term>
<term>SARS Virus (drug effects)</term>
<term>Structure-Activity Relationship</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en">
<term>Antiviral Agents</term>
<term>Pyridines</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en">
<term>Antiviral Agents</term>
<term>Pyridines</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en">
<term>Coronavirus, Feline</term>
<term>SARS Virus</term>
</keywords>
<keywords scheme="MESH" xml:lang="en">
<term>Animals</term>
<term>Cats</term>
<term>Cells, Cultured</term>
<term>Humans</term>
<term>Molecular Structure</term>
<term>Structure-Activity Relationship</term>
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<front>
<div type="abstract" xml:lang="en">Evaluation of a wide variety of pyridine N-oxide derivatives on their inhibitory activity against feline coronavirus (FIPV strain) and human SARS-CoV (Frankfurt strain-1) in cell culture.</div>
</front>
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<DateCompleted>
<Year>2006</Year>
<Month>05</Month>
<Day>10</Day>
</DateCompleted>
<DateRevised>
<Year>2020</Year>
<Month>04</Month>
<Day>03</Day>
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<ISSN IssnType="Print">0305-7453</ISSN>
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<Volume>57</Volume>
<Issue>3</Issue>
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<Year>2006</Year>
<Month>Mar</Month>
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</JournalIssue>
<Title>The Journal of antimicrobial chemotherapy</Title>
<ISOAbbreviation>J. Antimicrob. Chemother.</ISOAbbreviation>
</Journal>
<ArticleTitle>Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture.</ArticleTitle>
<Pagination>
<MedlinePgn>472-81</MedlinePgn>
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<AbstractText Label="OBJECTIVES" NlmCategory="OBJECTIVE">Evaluation of a wide variety of pyridine N-oxide derivatives on their inhibitory activity against feline coronavirus (FIPV strain) and human SARS-CoV (Frankfurt strain-1) in cell culture.</AbstractText>
<AbstractText Label="METHODS" NlmCategory="METHODS">FIPV and SARS-CoV were exposed to confluent Crandel feline kidney (CRFK) and simian kidney (Vero) cell cultures in the presence of serial concentrations of the test compounds. The anti-cytopathic activity of the pyridine N-oxide derivatives was monitored by spectrophotometric analysis.</AbstractText>
<AbstractText Label="RESULTS AND CONCLUSIONS" NlmCategory="CONCLUSIONS">A wide variety of pyridine N-oxide derivatives have been found to be inhibitory against feline coronavirus (FIPV strain) and human SARS-CoV (Frankfurt strain-1) in CRFK and simian kidney (Vero) cell cultures, respectively. The oxide part on the pyridine moiety proved indispensable for anti-coronavirus activity. The potency and virus specificity of the pyridine N-oxide derivatives varied depending the nature and specific location of substituents (i.e. alkyl, halogeno, nitro, etc.) on the different parts of the molecule. The most selective compounds were active in the higher microgram per litre range, being non-toxic at 50-100 mg/L. There was a poor structure-antiviral activity relationship (SAR) for the pyridine N-oxide derivatives against Fe-CoV and SARS-CoV. One of the most active and selective compounds was shown to inhibit Fe-CoV replication at the transcriptional level.</AbstractText>
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