About: Identification of 4-Anilino-6-aminoquinazoline Derivatives as Potential MERS-CoV Inhibitors

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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
has title	Identification of 4-Anilino-6-aminoquinazoline Derivatives as Potential MERS-CoV Inhibitors
Creator	Park, Min Kim, M Lee, Y Song, S Jin, S Kim, Rae Kwon, J Seong Jang, Y-H Sup Shin, J
Source	Elsevier; Medline; PMC
abstract	New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N(4)-(3-Chloro-4-fluorophenyl)-N(6)-(3-methoxybenzyl)quinazoline-4,6-diamine (1) has been identified in a random screen as a hit compound for inhibiting MERS-CoV infection. Throughout optimization process, compound 20 was found to exhibit high inhibitory effect (IC(50) = 0.157 μM, SI = 25) with no cytotoxicity and moderate in vivo PK properties.
has issue date	2020-08-08(xsd:dateTime)
bibo:doi	10.1016/j.bmcl.2020.127472
bibo:pmid	32781216
has license	no-cc
sha1sum (hex)	2920ed1db2dff60140dea0869d85d912d70b90e1
schema:url	https://doi.org/10.1016/j.bmcl.2020.127472
resource representing a document's title	Identification of 4-Anilino-6-aminoquinazoline Derivatives as Potential MERS-CoV Inhibitors
has PubMed Central identifier	PMC7414322
has PubMed identifier	32781216
schema:publication	Bioorg Med Chem Lett
resource representing a document's body	covid:2920ed1db2dff60140dea0869d85d912d70b90e1#body_text
is schema:about of	named entity 'derivatives' named entity 'NEW' named entity '283' named entity 'CORONAVIRUSES' named entity 'PROCESS' named entity 'SCREEN' named entity 'INHIBITORY EFFECT' named entity 'compound' named entity 'inhibitory' named entity 'evaluated' named entity 'coronaviruses' named entity 'cytotoxicity' named entity 'infection' named entity 'coronaviruses' named entity 'Anilino' named entity 'Lapatinib' named entity 'HCS' named entity 'animal reservoirs' named entity 'anticancer drugs' named entity 'IPK' named entity 'SARS-CoV-2' named entity 'infection' named entity 'severe acute respiratory syndrome' named entity 'Drug repositioning' named entity 'protein kinase' named entity 'coronaviruses' named entity 'epidermal growth factor receptor' named entity 'China' named entity '4 April 2020' named entity 'Gefitinib' named entity 'oral bioavailability' named entity 'FDA' named entity 'public health' named entity 'coronavirus' named entity 'substituent' named entity 'Erlotinib' named entity 'MERS-CoV' named entity 'infection' named entity 'infection' named entity 'phenyl ring' named entity 'metabolic stability' named entity 'Middle East respiratory syndrome' named entity 'MERS-CoV' named entity 'EGFR' named entity 'MERS-CoV' named entity 'MERS-CoV' named entity 'virus' named entity 'KCB' named entity 'cytotoxicity' named entity 'respiratory diseases' named entity 'coronaviruses' named entity 'Quinazoline' named entity 'infection' named entity 'SARS' named entity 'quinazoline' named entity 'MERS-CoV' named entity 'high content screening' named entity 'phenyl ring' named entity 'Institut Pasteur Korea' named entity 'SARS-CoV' named entity 'MERS-CoV' named entity 'COVID-19' named entity 'quinazoline' named entity 'bioavailability' named entity 'cytotoxicity' named entity 'MERS-CoV' named entity 'Afatinib' named entity 'quinazoline' named entity 'severe acute respiratory syndrome coronavirus 2' named entity 'hERG' named entity 'MERS-CoV' named entity 'MERS-CoV' named entity 'MERS-CoV'

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