Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture
Identifieur interne : 004196 ( Main/Exploration ); précédent : 004195; suivant : 004197Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture
Auteurs : Jan Balzarini [Belgique] ; Els Keyaerts [Belgique] ; Leen Vijgen [Belgique] ; Frank Vandermeer [Pays-Bas] ; Miguel Stevens [Belgique] ; Erik De Clercq [Belgique] ; Herman Egberink [Pays-Bas] ; Marc Van Ranst [Belgique]Source :
- Journal of Antimicrobial Chemotherapy [ 0305-7453 ] ; 2005.
Descripteurs français
- KwdFr :
- MESH :
- pharmacologie : Antiviraux, Pyridines.
- Animaux, Antiviraux, Cellules cultivées, Chats, Coronavirus félin, Humains, Pyridines, Relation structure-activité, Structure moléculaire, Virus du SRAS.
- Pascal (Inist)
- Wicri :
- topic : Homme.
English descriptors
- KwdEn :
- Animals, Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Cats, Cell culture, Cells, Cultured, Coronavirus, Coronavirus, Feline (drug effects), Feline infectious peritonitis, Human, Humans, In vitro, Molecular Structure, Pyridine derivatives, Pyridines (chemistry), Pyridines (pharmacology), SARS Virus (drug effects), Severe acute respiratory syndrome, Structure-Activity Relationship.
- MESH :
- chemical , chemistry : Antiviral Agents, Pyridines.
- chemical , pharmacology : Antiviral Agents, Pyridines.
- drug effects : Coronavirus, Feline, SARS Virus.
- Animals, Cats, Cells, Cultured, Humans, Molecular Structure, Structure-Activity Relationship.
Abstract
Objectives: 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. 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. Results and 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.
Url:
- https://api.istex.fr/ark:/67375/HXZ-SV6PL67X-H/fulltext.pdf
- http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7110042
DOI: 10.1093/jac/dki481
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream Istex, to step Corpus: 000147
- to stream Istex, to step Curation: 000147
- to stream Istex, to step Checkpoint: 001622
- to stream Pmc, to step Corpus: 001106
- to stream Pmc, to step Curation: 001106
- to stream Pmc, to step Checkpoint: 001266
- to stream PubMed, to step Corpus: 002389
- to stream PubMed, to step Curation: 002389
- to stream PubMed, to step Checkpoint: 002047
- to stream Ncbi, to step Merge: 001326
- to stream Ncbi, to step Curation: 001326
- to stream Ncbi, to step Checkpoint: 001326
- to stream Main, to step Merge: 004412
- to stream PascalFrancis, to step Corpus: 000506
- to stream PascalFrancis, to step Curation: 000484
- to stream PascalFrancis, to step Checkpoint: 000440
- to stream Main, to step Merge: 004641
- to stream Main, to step Curation: 004196
Le document en format XML
<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><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></author><author><name sortKey="Keyaerts, Els" sort="Keyaerts, Els" uniqKey="Keyaerts E" first="Els" last="Keyaerts">Els Keyaerts</name></author><author><name sortKey="Vijgen, Leen" sort="Vijgen, Leen" uniqKey="Vijgen L" first="Leen" last="Vijgen">Leen Vijgen</name></author><author><name sortKey="Vandermeer, Frank" sort="Vandermeer, Frank" uniqKey="Vandermeer F" first="Frank" last="Vandermeer">Frank Vandermeer</name></author><author><name sortKey="Stevens, Miguel" sort="Stevens, Miguel" uniqKey="Stevens M" first="Miguel" last="Stevens">Miguel Stevens</name></author><author><name sortKey="De Clercq, Erik" sort="De Clercq, Erik" uniqKey="De Clercq E" first="Erik" last="De Clercq">Erik De Clercq</name></author><author><name sortKey="Egberink, Herman" sort="Egberink, Herman" uniqKey="Egberink H" first="Herman" last="Egberink">Herman Egberink</name></author><author><name sortKey="Van Ranst, Marc" sort="Van Ranst, Marc" uniqKey="Van Ranst M" first="Marc" last="Van Ranst">Marc Van Ranst</name></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:204CE38B08442996116884669633748144B69C3A</idno><date when="2006" year="2006">2006</date><idno type="doi">10.1093/jac/dki481</idno><idno type="url">https://api.istex.fr/ark:/67375/HXZ-SV6PL67X-H/fulltext.pdf</idno><idno type="wicri:Area/Istex/Corpus">000147</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">000147</idno><idno type="wicri:Area/Istex/Curation">000147</idno><idno type="wicri:Area/Istex/Checkpoint">001622</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Checkpoint">001622</idno><idno type="wicri:doubleKey">0305-7453:2006:Balzarini J:pyridine:n:oxide</idno><idno type="wicri:source">PMC</idno><idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7110042</idno><idno type="RBID">PMC:7110042</idno><idno type="wicri:Area/Pmc/Corpus">001106</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">001106</idno><idno type="wicri:Area/Pmc/Curation">001106</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Curation">001106</idno><idno type="wicri:Area/Pmc/Checkpoint">001266</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Checkpoint">001266</idno><idno type="wicri:source">PubMed</idno><idno type="RBID">pubmed:16387746</idno><idno type="wicri:Area/PubMed/Corpus">002389</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">002389</idno><idno type="wicri:Area/PubMed/Curation">002389</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">002389</idno><idno type="wicri:Area/PubMed/Checkpoint">002047</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">002047</idno><idno type="wicri:Area/Ncbi/Merge">001326</idno><idno type="wicri:Area/Ncbi/Curation">001326</idno><idno type="wicri:Area/Ncbi/Checkpoint">001326</idno><idno type="wicri:Area/Main/Merge">004412</idno><idno type="wicri:source">INIST</idno><idno type="RBID">Pascal:06-0221426</idno><idno type="wicri:Area/PascalFrancis/Corpus">000506</idno><idno type="wicri:Area/PascalFrancis/Curation">000484</idno><idno type="wicri:Area/PascalFrancis/Checkpoint">000440</idno><idno type="wicri:explorRef" wicri:stream="PascalFrancis" wicri:step="Checkpoint">000440</idno><idno type="wicri:doubleKey">0305-7453:2006:Balzarini J:pyridine:n:oxide</idno><idno type="wicri:Area/Main/Merge">004641</idno><idno type="wicri:Area/Main/Curation">004196</idno><idno type="wicri:Area/Main/Exploration">004196</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a" type="main">Pyridine <hi rend="italic">N</hi>-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 wicri:level="1"><country xml:lang="fr" wicri:curation="lc">Belgique</country><wicri:regionArea>Rega Institute for Medical Research, K.U. Leuven, Leuven</wicri:regionArea><wicri:noRegion>Leuven</wicri:noRegion></affiliation><affiliation wicri:level="1"><country wicri:rule="url">Belgique</country></affiliation></author><author><name sortKey="Keyaerts, Els" sort="Keyaerts, Els" uniqKey="Keyaerts E" first="Els" last="Keyaerts">Els Keyaerts</name><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">Belgique</country><wicri:regionArea>Rega Institute for Medical Research, K.U. Leuven, Leuven</wicri:regionArea><wicri:noRegion>Leuven</wicri:noRegion></affiliation></author><author><name sortKey="Vijgen, Leen" sort="Vijgen, Leen" uniqKey="Vijgen L" first="Leen" last="Vijgen">Leen Vijgen</name><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">Belgique</country><wicri:regionArea>Rega Institute for Medical Research, K.U. Leuven, Leuven</wicri:regionArea><wicri:noRegion>Leuven</wicri:noRegion></affiliation></author><author><name sortKey="Vandermeer, Frank" sort="Vandermeer, Frank" uniqKey="Vandermeer F" first="Frank" last="Vandermeer">Frank Vandermeer</name><affiliation wicri:level="4"><country xml:lang="fr">Pays-Bas</country><wicri:regionArea>Institute of Virology, Faculty of Veterinary Medicine, Utrecht University, Utrecht</wicri:regionArea><placeName><settlement type="city">Utrecht</settlement><region nuts="2" type="province">Utrecht (province)</region></placeName><orgName type="university">Université d'Utrecht</orgName></affiliation></author><author><name sortKey="Stevens, Miguel" sort="Stevens, Miguel" uniqKey="Stevens M" first="Miguel" last="Stevens">Miguel Stevens</name><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">Belgique</country><wicri:regionArea>Rega Institute for Medical Research, K.U. Leuven, Leuven</wicri:regionArea><wicri:noRegion>Leuven</wicri:noRegion></affiliation></author><author><name sortKey="De Clercq, Erik" sort="De Clercq, Erik" uniqKey="De Clercq E" first="Erik" last="De Clercq">Erik De Clercq</name><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">Belgique</country><wicri:regionArea>Rega Institute for Medical Research, K.U. Leuven, Leuven</wicri:regionArea><wicri:noRegion>Leuven</wicri:noRegion></affiliation></author><author><name sortKey="Egberink, Herman" sort="Egberink, Herman" uniqKey="Egberink H" first="Herman" last="Egberink">Herman Egberink</name><affiliation wicri:level="4"><country xml:lang="fr">Pays-Bas</country><wicri:regionArea>Institute of Virology, Faculty of Veterinary Medicine, Utrecht University, Utrecht</wicri:regionArea><placeName><settlement type="city">Utrecht</settlement><region nuts="2" type="province">Utrecht (province)</region></placeName><orgName type="university">Université d'Utrecht</orgName></affiliation></author><author><name sortKey="Van Ranst, Marc" sort="Van Ranst, Marc" uniqKey="Van Ranst M" first="Marc" last="Van Ranst">Marc Van Ranst</name><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">Belgique</country><wicri:regionArea>Rega Institute for Medical Research, K.U. Leuven, Leuven</wicri:regionArea><wicri:noRegion>Leuven</wicri:noRegion></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Antimicrobial Chemotherapy</title><title level="j" type="abbrev">J. Antimicrob. Chemother.</title><idno type="ISSN">0305-7453</idno><idno type="eISSN">1460-2091</idno><imprint><publisher>Oxford University Press</publisher><date type="e-published">2005</date><date type="published">2006</date><biblScope unit="vol">57</biblScope><biblScope unit="issue">3</biblScope><biblScope unit="page" from="472">472</biblScope><biblScope unit="page" to="481">481</biblScope></imprint><idno type="ISSN">0305-7453</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0305-7453</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (pharmacology)</term><term>Cats</term><term>Cell culture</term><term>Cells, Cultured</term><term>Coronavirus</term><term>Coronavirus, Feline (drug effects)</term><term>Feline infectious peritonitis</term><term>Human</term><term>Humans</term><term>In vitro</term><term>Molecular Structure</term><term>Pyridine derivatives</term><term>Pyridines (chemistry)</term><term>Pyridines (pharmacology)</term><term>SARS Virus (drug effects)</term><term>Severe acute respiratory syndrome</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term><term>Antiviraux ()</term><term>Antiviraux (pharmacologie)</term><term>Cellules cultivées</term><term>Chats</term><term>Coronavirus félin ()</term><term>Humains</term><term>Pyridines ()</term><term>Pyridines (pharmacologie)</term><term>Relation structure-activité</term><term>Structure moléculaire</term><term>Virus du SRAS ()</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" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term><term>Pyridines</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></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Antiviraux</term><term>Cellules cultivées</term><term>Chats</term><term>Coronavirus félin</term><term>Humains</term><term>Pyridines</term><term>Relation structure-activité</term><term>Structure moléculaire</term><term>Virus du SRAS</term></keywords><keywords scheme="Pascal" xml:lang="fr"><term>Coronavirus</term><term>Culture cellulaire</term><term>Homme</term><term>In vitro</term><term>Pyridine dérivé</term><term>Péritonite infectieuse féline</term><term>Syndrome respiratoire aigu sévère</term></keywords><keywords scheme="Wicri" type="topic" xml:lang="fr"><term>Homme</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Objectives: 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. 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. Results and 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.</div></front></TEI><affiliations><list><country><li>Belgique</li><li>Pays-Bas</li></country><region><li>Utrecht (province)</li></region><settlement><li>Utrecht</li></settlement><orgName><li>Université d'Utrecht</li></orgName></list><tree><country name="Belgique"><noRegion><name sortKey="Balzarini, Jan" sort="Balzarini, Jan" uniqKey="Balzarini J" first="Jan" last="Balzarini">Jan Balzarini</name></noRegion><name sortKey="Balzarini, Jan" sort="Balzarini, Jan" uniqKey="Balzarini J" first="Jan" last="Balzarini">Jan Balzarini</name><name sortKey="De Clercq, Erik" sort="De Clercq, Erik" uniqKey="De Clercq E" first="Erik" last="De Clercq">Erik De Clercq</name><name sortKey="Keyaerts, Els" sort="Keyaerts, Els" uniqKey="Keyaerts E" first="Els" last="Keyaerts">Els Keyaerts</name><name sortKey="Stevens, Miguel" sort="Stevens, Miguel" uniqKey="Stevens M" first="Miguel" last="Stevens">Miguel Stevens</name><name sortKey="Van Ranst, Marc" sort="Van Ranst, Marc" uniqKey="Van Ranst M" first="Marc" last="Van Ranst">Marc Van Ranst</name><name sortKey="Vijgen, Leen" sort="Vijgen, Leen" uniqKey="Vijgen L" first="Leen" last="Vijgen">Leen Vijgen</name></country><country name="Pays-Bas"><region name="Utrecht (province)"><name sortKey="Vandermeer, Frank" sort="Vandermeer, Frank" uniqKey="Vandermeer F" first="Frank" last="Vandermeer">Frank Vandermeer</name></region><name sortKey="Egberink, Herman" sort="Egberink, Herman" uniqKey="Egberink H" first="Herman" last="Egberink">Herman Egberink</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/SrasV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 004196 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 004196 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Sante
|area= SrasV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= ISTEX:204CE38B08442996116884669633748144B69C3A
|texte= Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture
}}
| This area was generated with Dilib version V0.6.33. |  |