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Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.

Identifieur interne : 000392 ( PubMed/Corpus ); précédent : 000391; suivant : 000393

Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.

Auteurs : Ji Hye Yoon ; Jun Young Lee ; Jihye Lee ; Young Sup Shin ; Sangeun Jeon ; Dong Eon Kim ; Jung Sun Min ; Jong Hwan Song ; Seungtaek Kim ; Sunoh Kwon ; Young-Hee Jin ; Min Seong Jang ; Hyoung Rae Kim ; Chul Min Park

Source :

RBID : pubmed:31624041

Abstract

3-Acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-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(1H)-one (6u) exhibits high inhibitory effect (IC50 = 86 nM) and low toxicity (CC50 > 25 μM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good in vivo PK properties.

DOI: 10.1016/j.bmcl.2019.126727
PubMed: 31624041

Links to Exploration step

pubmed:31624041

Le document en format XML

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<name sortKey="Kim, Dong Eon" sort="Kim, Dong Eon" uniqKey="Kim D" first="Dong Eon" last="Kim">Dong Eon Kim</name>
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<name sortKey="Min, Jung Sun" sort="Min, Jung Sun" uniqKey="Min J" first="Jung Sun" last="Min">Jung Sun Min</name>
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<name sortKey="Song, Jong Hwan" sort="Song, Jong Hwan" uniqKey="Song J" first="Jong Hwan" last="Song">Jong Hwan Song</name>
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<name sortKey="Kim, Seungtaek" sort="Kim, Seungtaek" uniqKey="Kim S" first="Seungtaek" last="Kim">Seungtaek Kim</name>
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<name sortKey="Kwon, Sunoh" sort="Kwon, Sunoh" uniqKey="Kwon S" first="Sunoh" last="Kwon">Sunoh Kwon</name>
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</affiliation>
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<name sortKey="Jin, Young Hee" sort="Jin, Young Hee" uniqKey="Jin Y" first="Young-Hee" last="Jin">Young-Hee Jin</name>
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<nlm:affiliation>Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea.</nlm:affiliation>
</affiliation>
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<name sortKey="Jang, Min Seong" sort="Jang, Min Seong" uniqKey="Jang M" first="Min Seong" last="Jang">Min Seong Jang</name>
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<nlm:affiliation>Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea.</nlm:affiliation>
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<name sortKey="Kim, Hyoung Rae" sort="Kim, Hyoung Rae" uniqKey="Kim H" first="Hyoung Rae" last="Kim">Hyoung Rae Kim</name>
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<front>
<div type="abstract" xml:lang="en">3-Acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-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(1H)-one (6u) 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 in vivo PK properties.</div>
</front>
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<ArticleTitle>Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.</ArticleTitle>
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<AbstractText>3-Acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-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(1H)-one (6u) exhibits high inhibitory effect (IC
<sub>50</sub>
 = 86 nM) and low toxicity (CC
<sub>50</sub>
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<Author ValidYN="Y">
<LastName>Yoon</LastName>
<ForeName>Ji Hye</ForeName>
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   |type=    RBID
   |clé=     pubmed:31624041
   |texte=   Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.
}}

Pour générer des pages wiki

HfdIndexSelect -h $EXPLOR_AREA/Data/PubMed/Corpus/RBID.i   -Sk "pubmed:31624041" \
       | HfdSelect -Kh $EXPLOR_AREA/Data/PubMed/Corpus/biblio.hfd   \
       | NlmPubMed2Wicri -a MersV1 

Wicri

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