Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors
Identifieur interne : 000162 ( Pmc/Checkpoint ); précédent : 000161; suivant : 000163Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors
Auteurs : Ji Hye Yoon [Corée du Sud] ; Jun Young Lee [Corée du Sud] ; Jihye Lee [Corée du Sud] ; Young Sup Shin [Corée du Sud] ; Sangeun Jeon [Corée du Sud] ; Dong Eon Kim [Corée du Sud] ; Jung Sun Min [Corée du Sud] ; Jong Hwan Song [Corée du Sud] ; Seungtaek Kim [Corée du Sud] ; Sunoh Kwon [Corée du Sud] ; Young-Hee Jin [Corée du Sud] ; Min Seong Jang [Corée du Sud] ; Hyoung Rae Kim [Corée du Sud] ; Chul Min Park [Corée du Sud]Source :
- Bioorganic & Medicinal Chemistry Letters [ 0960-894X ] ; 2019.
Abstract
Url:
DOI: 10.1016/j.bmcl.2019.126727
PubMed: 31624041
PubMed Central: 7126094
Affiliations:
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1<italic>H</italic>)-one derivatives as potential MERS-CoV inhibitors</title><author><name sortKey="Yoon, Ji Hye" sort="Yoon, Ji Hye" uniqKey="Yoon J" first="Ji Hye" last="Yoon">Ji Hye Yoon</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Lee, Jun Young" sort="Lee, Jun Young" uniqKey="Lee J" first="Jun Young" last="Lee">Jun Young Lee</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Lee, Jihye" sort="Lee, Jihye" uniqKey="Lee J" first="Jihye" last="Lee">Jihye Lee</name><affiliation wicri:level="1"><nlm:aff id="af010">Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488</wicri:regionArea><wicri:noRegion>Gyeonggi-do 13488</wicri:noRegion></affiliation></author><author><name sortKey="Shin, Young Sup" sort="Shin, Young Sup" uniqKey="Shin Y" first="Young Sup" last="Shin">Young Sup Shin</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Jeon, Sangeun" sort="Jeon, Sangeun" uniqKey="Jeon S" first="Sangeun" last="Jeon">Sangeun Jeon</name><affiliation wicri:level="1"><nlm:aff id="af010">Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488</wicri:regionArea><wicri:noRegion>Gyeonggi-do 13488</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Dong Eon" sort="Kim, Dong Eon" uniqKey="Kim D" first="Dong Eon" last="Kim">Dong Eon Kim</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Min, Jung Sun" sort="Min, Jung Sun" uniqKey="Min J" first="Jung Sun" last="Min">Jung Sun Min</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Song, Jong Hwan" sort="Song, Jong Hwan" uniqKey="Song J" first="Jong Hwan" last="Song">Jong Hwan Song</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Seungtaek" sort="Kim, Seungtaek" uniqKey="Kim S" first="Seungtaek" last="Kim">Seungtaek Kim</name><affiliation wicri:level="1"><nlm:aff id="af020">Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488</wicri:regionArea><wicri:noRegion>Gyeonggi-do 13488</wicri:noRegion></affiliation></author><author><name sortKey="Kwon, Sunoh" sort="Kwon, Sunoh" uniqKey="Kwon S" first="Sunoh" last="Kwon">Sunoh Kwon</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Jin, Young Hee" sort="Jin, Young Hee" uniqKey="Jin Y" first="Young-Hee" last="Jin">Young-Hee Jin</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Jang, Min Seong" sort="Jang, Min Seong" uniqKey="Jang M" first="Min Seong" last="Jang">Min Seong Jang</name><affiliation wicri:level="1"><nlm:aff id="af025">Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Hyoung Rae" sort="Kim, Hyoung Rae" uniqKey="Kim H" first="Hyoung Rae" last="Kim">Hyoung Rae Kim</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Park, Chul Min" sort="Park, Chul Min" uniqKey="Park C" first="Chul Min" last="Park">Chul Min Park</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PMC</idno><idno type="pmid">31624041</idno><idno type="pmc">7126094</idno><idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126094</idno><idno type="RBID">PMC:7126094</idno><idno type="doi">10.1016/j.bmcl.2019.126727</idno><date when="2019">2019</date><idno type="wicri:Area/Pmc/Corpus">000663</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">000663</idno><idno 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Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Lee, Jun Young" sort="Lee, Jun Young" uniqKey="Lee J" first="Jun Young" last="Lee">Jun Young Lee</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Lee, Jihye" sort="Lee, Jihye" uniqKey="Lee J" first="Jihye" last="Lee">Jihye Lee</name><affiliation wicri:level="1"><nlm:aff id="af010">Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488</wicri:regionArea><wicri:noRegion>Gyeonggi-do 13488</wicri:noRegion></affiliation></author><author><name sortKey="Shin, Young Sup" sort="Shin, Young Sup" uniqKey="Shin Y" first="Young Sup" last="Shin">Young Sup Shin</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Jeon, Sangeun" sort="Jeon, Sangeun" uniqKey="Jeon S" first="Sangeun" last="Jeon">Sangeun Jeon</name><affiliation wicri:level="1"><nlm:aff id="af010">Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488</wicri:regionArea><wicri:noRegion>Gyeonggi-do 13488</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Dong Eon" sort="Kim, Dong Eon" uniqKey="Kim D" first="Dong Eon" last="Kim">Dong Eon Kim</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Min, Jung Sun" sort="Min, Jung Sun" uniqKey="Min J" first="Jung Sun" last="Min">Jung Sun Min</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Song, Jong Hwan" sort="Song, Jong Hwan" uniqKey="Song J" first="Jong Hwan" last="Song">Jong Hwan Song</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Seungtaek" sort="Kim, Seungtaek" uniqKey="Kim S" first="Seungtaek" last="Kim">Seungtaek Kim</name><affiliation wicri:level="1"><nlm:aff id="af020">Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488</wicri:regionArea><wicri:noRegion>Gyeonggi-do 13488</wicri:noRegion></affiliation></author><author><name sortKey="Kwon, Sunoh" sort="Kwon, Sunoh" uniqKey="Kwon S" first="Sunoh" last="Kwon">Sunoh Kwon</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Jin, Young Hee" sort="Jin, Young Hee" uniqKey="Jin Y" first="Young-Hee" last="Jin">Young-Hee Jin</name><affiliation wicri:level="1"><nlm:aff id="af015">Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054</wicri:regionArea><wicri:noRegion>Daejeon 34054</wicri:noRegion></affiliation></author><author><name sortKey="Jang, Min Seong" sort="Jang, Min Seong" uniqKey="Jang M" first="Min Seong" last="Jang">Min Seong Jang</name><affiliation wicri:level="1"><nlm:aff id="af025">Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Hyoung Rae" sort="Kim, Hyoung Rae" uniqKey="Kim H" first="Hyoung Rae" last="Kim">Hyoung Rae Kim</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author><author><name sortKey="Park, Chul Min" sort="Park, Chul Min" uniqKey="Park C" first="Chul Min" last="Park">Chul Min Park</name><affiliation wicri:level="1"><nlm:aff id="af005">Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</nlm:aff><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114</wicri:regionArea><wicri:noRegion>Daejeon 34114</wicri:noRegion></affiliation></author></analytic><series><title level="j">Bioorganic & Medicinal Chemistry Letters</title><idno type="ISSN">0960-894X</idno><idno type="eISSN">1464-3405</idno><imprint><date 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<front><journal-meta><journal-id journal-id-type="nlm-ta">Bioorg Med Chem Lett</journal-id><journal-id journal-id-type="iso-abbrev">Bioorg. Med. Chem. Lett</journal-id><journal-title-group><journal-title>Bioorganic & Medicinal Chemistry Letters</journal-title></journal-title-group><issn pub-type="ppub">0960-894X</issn><issn pub-type="epub">1464-3405</issn><publisher><publisher-name>Elsevier Ltd.</publisher-name></publisher></journal-meta><article-meta><article-id pub-id-type="pmid">31624041</article-id><article-id pub-id-type="pmc">7126094</article-id><article-id pub-id-type="publisher-id">S0960-894X(19)30685-7</article-id><article-id pub-id-type="doi">10.1016/j.bmcl.2019.126727</article-id><article-id pub-id-type="publisher-id">126727</article-id><article-categories><subj-group subj-group-type="heading"><subject>Article</subject></subj-group></article-categories><title-group><article-title>Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1<italic>H</italic>)-one derivatives as potential MERS-CoV inhibitors</article-title></title-group><contrib-group><contrib contrib-type="author" id="au005"><name><surname>Yoon</surname><given-names>Ji Hye</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au010"><name><surname>Lee</surname><given-names>Jun Young</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au015"><name><surname>Lee</surname><given-names>Jihye</given-names></name><xref rid="af010" ref-type="aff">b</xref></contrib><contrib contrib-type="author" id="au020"><name><surname>Shin</surname><given-names>Young Sup</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au025"><name><surname>Jeon</surname><given-names>Sangeun</given-names></name><xref rid="af010" ref-type="aff">b</xref></contrib><contrib contrib-type="author" id="au030"><name><surname>Kim</surname><given-names>Dong Eon</given-names></name><xref rid="af015" ref-type="aff">c</xref></contrib><contrib contrib-type="author" id="au035"><name><surname>Min</surname><given-names>Jung Sun</given-names></name><xref rid="af015" ref-type="aff">c</xref></contrib><contrib contrib-type="author" id="au040"><name><surname>Song</surname><given-names>Jong Hwan</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au045"><name><surname>Kim</surname><given-names>Seungtaek</given-names></name><xref rid="af020" ref-type="aff">d</xref></contrib><contrib contrib-type="author" id="au050"><name><surname>Kwon</surname><given-names>Sunoh</given-names></name><xref rid="af015" ref-type="aff">c</xref></contrib><contrib contrib-type="author" id="au055"><name><surname>Jin</surname><given-names>Young-hee</given-names></name><xref rid="af015" ref-type="aff">c</xref></contrib><contrib contrib-type="author" id="au060"><name><surname>Jang</surname><given-names>Min Seong</given-names></name><xref rid="af025" ref-type="aff">e</xref></contrib><contrib contrib-type="author" id="au065"><name><surname>Kim</surname><given-names>Hyoung Rae</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au070"><name><surname>Park</surname><given-names>Chul Min</given-names></name><xref rid="af005" ref-type="aff">a</xref><xref rid="cor1" ref-type="corresp">⁎</xref></contrib></contrib-group><aff id="af005"><label>a</label>Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea</aff><aff id="af010"><label>b</label>Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</aff><aff id="af015"><label>c</label>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea</aff><aff id="af020"><label>d</label>Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea</aff><aff id="af025"><label>e</label>Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea</aff><author-notes><corresp id="cor1"><label>⁎</label>Corresponding author.</corresp></author-notes><pub-date pub-type="pmc-release"><day>9</day><month>10</month><year>2019</year></pub-date><pmc-comment> PMC Release delay is 0 months and 0 days and was based on .</pmc-comment>
<pub-date pub-type="ppub"><day>1</day><month>12</month><year>2019</year></pub-date><pub-date pub-type="epub"><day>9</day><month>10</month><year>2019</year></pub-date><volume>29</volume><issue>23</issue><fpage>126727</fpage><lpage>126727</lpage><history><date date-type="received"><day>24</day><month>6</month><year>2019</year></date><date date-type="rev-recd"><day>6</day><month>9</month><year>2019</year></date><date date-type="accepted"><day>30</day><month>9</month><year>2019</year></date></history><permissions><copyright-statement>© 2019 Elsevier Ltd. All rights reserved.</copyright-statement><copyright-year>2019</copyright-year><copyright-holder>Elsevier Ltd</copyright-holder><license><license-p>Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.</license-p></license></permissions><abstract abstract-type="graphical" id="ab005"><title>Graphical abstract</title><fig id="f0020" position="anchor"><graphic xlink:href="ga1_lrg"></graphic></fig></abstract><abstract id="ab010"><p>3-Acyl-2-phenylamino-1,4-dihydroquinolin-4(1<italic>H</italic>)-one derivatives were synthesized and evaluated to show high anti-MERS-CoV inhibitory activities. Among them, 6,8-difluoro-3-isobutyryl-2-((2,3,4-trifluorophenyl)amino)quinolin-4(1<italic>H</italic>)-one (<bold>6u</bold>) exhibits high inhibitory effect (IC<sub>50</sub> = 86 nM) and low toxicity (CC<sub>50</sub> > 25 μM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good <italic>in vivo</italic> PK properties.</p></abstract><kwd-group id="kg005"><title>Keywords</title><kwd>MERS-CoV</kwd><kwd>RNA virus</kwd><kwd>3-Acyl-2-amino-1,4-dihydroquinolin-4(1<italic>H</italic>)-ones</kwd><kwd>Inhibitor</kwd><kwd>SAR optimization</kwd></kwd-group></article-meta></front></pmc><affiliations><list><country><li>Corée du Sud</li></country></list><tree><country name="Corée du Sud"><noRegion><name sortKey="Yoon, Ji Hye" sort="Yoon, Ji Hye" uniqKey="Yoon J" first="Ji Hye" last="Yoon">Ji Hye Yoon</name></noRegion><name sortKey="Jang, Min Seong" sort="Jang, Min Seong" uniqKey="Jang M" first="Min Seong" last="Jang">Min Seong Jang</name><name sortKey="Jeon, Sangeun" sort="Jeon, Sangeun" uniqKey="Jeon S" first="Sangeun" last="Jeon">Sangeun Jeon</name><name sortKey="Jin, Young Hee" sort="Jin, Young Hee" uniqKey="Jin Y" first="Young-Hee" last="Jin">Young-Hee Jin</name><name sortKey="Kim, Dong Eon" sort="Kim, Dong Eon" uniqKey="Kim D" first="Dong Eon" last="Kim">Dong Eon Kim</name><name sortKey="Kim, Hyoung Rae" sort="Kim, Hyoung Rae" uniqKey="Kim H" first="Hyoung Rae" last="Kim">Hyoung Rae Kim</name><name sortKey="Kim, Seungtaek" sort="Kim, Seungtaek" uniqKey="Kim S" first="Seungtaek" last="Kim">Seungtaek Kim</name><name sortKey="Kwon, Sunoh" sort="Kwon, Sunoh" uniqKey="Kwon S" first="Sunoh" last="Kwon">Sunoh Kwon</name><name sortKey="Lee, Jihye" sort="Lee, Jihye" uniqKey="Lee J" first="Jihye" last="Lee">Jihye Lee</name><name sortKey="Lee, Jun Young" sort="Lee, Jun Young" uniqKey="Lee J" first="Jun Young" last="Lee">Jun Young Lee</name><name sortKey="Min, Jung Sun" sort="Min, Jung Sun" uniqKey="Min J" first="Jung Sun" last="Min">Jung Sun Min</name><name sortKey="Park, Chul Min" sort="Park, Chul Min" uniqKey="Park C" first="Chul Min" last="Park">Chul Min Park</name><name sortKey="Shin, Young Sup" sort="Shin, Young Sup" uniqKey="Shin Y" first="Young Sup" last="Shin">Young Sup Shin</name><name sortKey="Song, Jong Hwan" sort="Song, Jong Hwan" uniqKey="Song J" first="Jong Hwan" last="Song">Jong Hwan Song</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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