About: New Isoxazolidine-Conjugates of Quinazolinones—Synthesis, Antiviral and Cytostatic Activity

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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
title	New Isoxazolidine-Conjugates of Quinazolinones—Synthesis, Antiviral and Cytostatic Activity
Creator	Schols, Dominique Andrei, Graciela Snoeck, Robert Grabkowska-Drużyc, Magdalena Piotrowska, Dorota
source	Medline; PMC
abstract	A novel series of (3-diethoxyphosphoryl)isoxazolidines substituted at C5 with various quinazolinones have been synthesized by the 1,3-dipolar cycloaddition of N-methyl-C-(diethoxyphosphoryl)nitrone with N3-substitued 2-vinyl-3H-quinazolin-4-ones. All isoxazolidines were assessed for antiviral activity against a broad range of DNA and RNA viruses. Isoxazolidines trans-11f/cis-11f (90:10), trans-11h and trans-11i/cis-11i (97:3) showed weak activity (EC(50) = 6.84, 15.29 and 9.44 μM) toward VZV (TK(+) strain) which was only one order of magnitude lower than that of acyclovir used as a reference drug. Phosphonates trans-11b/cis-11b (90:10), trans-11c, trans-11e/cis-11e (90:10) and trans-11g appeared slightly active toward cytomegalovirus (EC(50) = 27–45 μM). Compounds containing benzyl substituents at N3 in the quinazolinone skeleton exhibited slight antiproliferative activity towards the tested immortalized cells with IC(50) in the 21–102 μM range.
has issue date	2016-07-22(xsd:dateTime)
bibo:doi	10.3390/molecules21070959
bibo:pmid	27455228
has license	cc-by
sha1sum (hex)	eefddcf51f8426ecaa9e3ace144dadfb34a74cf5
schema:url	https://doi.org/10.3390/molecules21070959
resource representing a document's title	New Isoxazolidine-Conjugates of Quinazolinones—Synthesis, Antiviral and Cytostatic Activity
has PubMed Central identifier	PMC6273226
has PubMed identifier	27455228
schema:publication	Molecules
resource representing a document's body	covid:eefddcf51f8426ecaa9e3ace144dadfb34a74cf5#body_text
is schema:about of	named entity 'DIPOLAR CYCLOADDITION' named entity 'REFERENCE' named entity '283' named entity 'ORDER' named entity 'CYTOSTATIC' named entity 'N-METHYL' covid:arg/eefddcf51f8426ecaa9e3ace144dadfb34a74cf5 named entity 'SLIGHT' named entity 'RNA VIRUSES' named entity 'MAGNITUDE' named entity 'DRUG' named entity 'HAVE' named entity 'SYNTHESIZED' named entity 'CONTAINING' named entity 'MOLECULES' named entity 'VINYL' named entity 'ASSESSED' named entity 'DNA' named entity 'ANTIVIRAL ACTIVITY' named entity 'ANTIVIRAL' named entity 'ACTIVITY' named entity 'ISOXAZOLIDINE' named entity 'NEW' named entity 'QUINAZOLINONES' named entity 'IMMORTALIZED' named entity 'NOVEL' named entity 'CELLS' named entity 'SERIES' named entity 'SKELETON' named entity 'VZV' named entity 'LOWER' named entity 'BENZYL' named entity 'TESTED' named entity '102' named entity 'ACYCLOVIR' named entity 'QUINAZOLINONES' named entity 'N3-' named entity '11I' named entity 'CYTOMEGALOVIRUS' named entity 'TRANS' named entity 'BROAD' named entity 'RANGE' named entity 'WEAK' named entity 'STRAIN' named entity 'SLIGHTLY' named entity 'VARIOUS' named entity 'ANTIPROLIFERATIVE ACTIVITY' named entity 'USED' named entity 'PHOSPHONATES' named entity 'SYNTHESIS' named entity 'CONJUGATES' named entity 'ACTIVITY' named entity 'ACTIVE' named entity 'trans' named entity 'viruses' named entity 'antiviral activity' named entity 'cytomegalovirus' named entity 'trans' named entity 'order of magnitude' named entity 'acyclovir' named entity 'biological activity' named entity 'cis' named entity 'mycophenolic acid' named entity 'Nitrogen-containing heterocycles' named entity 'trans' named entity 'trans' named entity 'Amorphous solid' named entity 'Hippeastrum' named entity 'alovudine' named entity 'phosphonates' named entity 'cis' named entity 'Urtica dioica' named entity 'H-NMR' named entity 'trans' named entity 'acyclovir' named entity 'antifungal' named entity 'nitrone'

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