About: SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase

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Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.benthamdirect.org/pages/b_viewarticle.php?articleID=3177425
Description	The current treatment of organophosphorus compounds induced intoxication consists of combined administration of anticholinergic drug, oxime reactivator and anticonvulsant. Oxime reactivators are causal treatment of organophosphorus intoxication and they are able to cleave OP moiety from the molecule of inhibited acetylcholinesterase. Unfortunately, none of the currently used oximes is sufficiently effective against all nerve agents and pesticides. Thus, finding of new potent acetylcholinesterase reactivators is necessary. In this study, the reactivation efficacy of three series of novel bisquaternary reactivators with prop-1,3-diyl, but-1,4-diyl and but-2-ene-1,4-diyl linker against paraoxon inhibited acetylcholinesterase in vitro is presented. The obtained results were compared to the commercially used reactivators (pralidoxime, trimedoxime, obidoxime, methoxime, asoxime). Some newly prepared compounds showed promising ability of paraoxon in vitro reactivation, even in human attainable plasma concentrations. The structure-activity relationship for reactivators of paraoxon induced inhibition was determined. The current treatment of organophosphorus compounds induced intoxication consists of combined administration of anticholinergic drug, oxime reactivator and anticonvulsant. Oxime reactivators are causal treatment of organophosphorus intoxication and they are able to cleave OP moiety from the molecule of inhibited acetylcholinesterase. Unfortunately, none of the currently used oximes is sufficiently effective against all nerve agents and pesticides. Thus, finding of new potent acetylcholinesterase reactivators is necessary. In this study, the reactivation efficacy of three series of novel bisquaternary reactivators with prop-1,3-diyl, but-1,4-diyl and but-2-ene-1,4-diyl linker against paraoxon inhibited acetylcholinesterase in vitro is presented. The obtained results were compared to the commercially used reactivators (pralidoxime, trimedoxime, obidoxime, methoxime, asoxime). Some newly prepared compounds showed promising ability of paraoxon in vitro reactivation, even in human attainable plasma concentrations. The structure-activity relationship for reactivators of paraoxon induced inhibition was determined. (en)
Title	SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase (en)
skos:prefLabel	SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase (en)
skos:notation	RIV/00179906:_____/12:10124634!RIV13-MZ0-00179906
http://linked.open...avai/predkladatel	Fakultní nemocnice Hradec Králové
http://linked.open...avai/riv/aktivita	I P S
http://linked.open...avai/riv/aktivity	I, P(ME09086), S
http://linked.open...iv/cisloPeriodika	6
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Kuča, Kamil
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Fakultní nemocnice Hradec Králové
http://linked.open...dnocenehoVysledku	166729
http://linked.open...ai/riv/idVysledku	RIV/00179906:_____/12:10124634
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	SAR; Oxime; Reactivator; Paraoxon; Organophosphate; Acetylcholinesterase (en)
http://linked.open.../riv/klicoveSlovo	Acetylcholinesterase SAR Reactivator Paraoxon Organophosphate Oxime
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[3C0CBBC062A6]
http://linked.open...i/riv/nazevZdroje	Letters in Drug Design and Discovery
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	1 (xsd:int)
http://linked.open...cetTvurcuVysledku	5 (xsd:int)
http://linked.open...vavai/riv/projekt	Development of novel antidotal treatment against organophosphorus pesticides
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	9
http://linked.open...iv/tvurceVysledku	Kuča, Kamil Musílek, Kamil Opletalová, Veronika Holas, Ondřej Horová, Anna
http://linked.open...ain/vavai/riv/wos	000308697100005
issn	1570-1808
number of pages	8 (xsd:int)
is http://linked.open...avai/riv/vysledek of	SAR Study on Reactivators of Ethyl-Paraoxon Inhibited Acetylcholinesterase

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