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

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About: Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors
Creator	Jin, Young-Hee Kim, Seungtaek Kwon, Sunoh Jeon, Sangeun Lee, Jihye Lee, Jun Park, Min Jang, Min Kim, Dong Kim, Hyoung Min, Jung Shin, Young Song, Jong Yoon, J Yoon, Ji
source	Elsevier; Medline; PMC
abstract	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.
has issue date	2019-12-01(xsd:dateTime)
bibo:doi	10.1016/j.bmcl.2019.126727
bibo:pmid	31624041
has license	els-covid
sha1sum (hex)	87c86810006f4b78602d0388d01a831de81bd52e
schema:url	https://doi.org/10.1016/j.bmcl.2019.126727
resource representing a document's title	Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors
has PubMed Central identifier	PMC7126094
has PubMed identifier	31624041
schema:publication	Bioorganic & Medicinal Chemistry Letters
resource representing a document's body	covid:87c86810006f4b78602d0388d01a831de81bd52e#body_text
is schema:about of	named entity 'MERS-COV' named entity 'PHENYLAMINO' named entity 'POTENTIAL' covid:arg/87c86810006f4b78602d0388d01a831de81bd52e named entity 'SYNTHESIS' named entity '2C4' named entity 'INHIBITORS' named entity 'R T' named entity 'BIOLOGICAL EVALUATION' named entity 'inhibitors' named entity 'acyl' named entity 'positive-sense RNA' named entity 'lead compound' named entity 'Dichlorobenzyl alcohol' named entity 'electron donating groups' named entity 'acetyl group' named entity 'virus' named entity 'neurodegenerative' named entity 'cytotoxicity' named entity 'Refluxing' named entity 'substituent' named entity 'binding affinities' named entity 'rat' named entity '4-chloroaniline' named entity 'pharmacological activities' named entity 'virion' named entity 'substitution reaction' named entity 'animal models' named entity 'MERS-CoV' named entity 'oral bioavailability' named entity 'genome replication' named entity 'aniline' named entity '3T3' named entity 'cytotoxicity' named entity 'high fever' named entity 'zoonotic' named entity 'dimethylsulfate' named entity 'trichloro' named entity 'acyl' named entity 'MERS-CoV' named entity 'carbon disulfide' named entity 'condensation reaction' named entity 'substituent' named entity 'cytotoxicity' named entity 'virus' named entity 'IPK' named entity 'KCB' named entity 'microsomes' named entity 'substituent' named entity 'acetyl' named entity 'HCS' named entity 'acyl' named entity '4-Bromoaniline' named entity 'hERG' named entity 'cell lines' named entity 'quinolone' named entity 'pharmacokinetic profile' named entity 'nitro' named entity 'acetyl acetate' named entity 'anilines' named entity 'L929' named entity 'phenyl' named entity 'binding affinity' named entity 'substituent' named entity 'RNA replication' named entity 'Vero cells' named entity 'amine'

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