About: A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) are able to treat intoxication by organophosphorus compounds,especially with pesticides or nerve agents. Owing to the fact that there exists no universal #broad-spectrum# reactivator oforganophosphates-inhibited AChE, many laboratories have synthesized new AChE reactivators. Here, we synthesized fivenew and three previously known quaternary monopyridinium oximes as potential reactivators of AChE inhibited by nerveagents. Potencies to cleave p-nitrophenyl acetate (PNPA), which is commonly used as a model substrate of nerve agents, were measured. Their cleaving potencies were compared with 4-PAM (4-hydroxyiminomethyl-1-methylpyridinium iodide), which is derived from the structure of the currently used AChE-reactivator 2-PAM (2-hydroxyiminomethyl-1-methylpyridiniumiodide). Three newly synthesized oximes achieved similar nucleophilicity at the similar pKa according to 4-PAM, which is very promising for using these derivatives as AChE reactivators. Reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) are able to treat intoxication by organophosphorus compounds,especially with pesticides or nerve agents. Owing to the fact that there exists no universal #broad-spectrum# reactivator oforganophosphates-inhibited AChE, many laboratories have synthesized new AChE reactivators. Here, we synthesized fivenew and three previously known quaternary monopyridinium oximes as potential reactivators of AChE inhibited by nerveagents. Potencies to cleave p-nitrophenyl acetate (PNPA), which is commonly used as a model substrate of nerve agents, were measured. Their cleaving potencies were compared with 4-PAM (4-hydroxyiminomethyl-1-methylpyridinium iodide), which is derived from the structure of the currently used AChE-reactivator 2-PAM (2-hydroxyiminomethyl-1-methylpyridiniumiodide). Three newly synthesized oximes achieved similar nucleophilicity at the similar pKa according to 4-PAM, which is very promising for using these derivatives as AChE reactivators. (en) Byly sytetizovány nové typy kvarterních pyridiniových ketoximů, jejichž účinnost byla testována na modelových substrátech. (cs)
Title	A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents Nové monokvarterní reaktivátory acetylcholinesterázy inhibované nervovými jedy (cs) A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents (en)
skos:prefLabel	A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents Nové monokvarterní reaktivátory acetylcholinesterázy inhibované nervovými jedy (cs) A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents (en)
skos:notation	RIV/60461373:22310/05:00013840!RIV06-MSM-22310___
http://linked.open.../vavai/riv/strany	233-237
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(GA203/01/1093), Z(MSM 223100001)
http://linked.open...iv/cisloPeriodika	3
http://linked.open...vai/riv/dodaniDat	2006
http://linked.open...aciTvurceVysledku	Liška, František Pícha, Jan
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	Vysoká škola chemicko-technologická v Praze / Fakulta chemické technologie
http://linked.open...dnocenehoVysledku	510946
http://linked.open...ai/riv/idVysledku	RIV/60461373:22310/05:00013840
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Acetylcholinesterase; Reactivator; PNPA; Reactivation; Verve agents; Inhibition (en)
http://linked.open.../riv/klicoveSlovo	PNPA Inhibition Reactivation Acetylcholinesterase Reactivator Verve agents
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[8F2FF97D19DE]
http://linked.open...i/riv/nazevZdroje	Journal of Enzyme Inhibition and Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CC
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	6 (xsd:int)
http://linked.open...vavai/riv/projekt	The effect of electron distribution on the oxime reactivity towards esters
http://linked.open...UplatneniVysledku	2005
http://linked.open...v/svazekPeriodika	20
http://linked.open...iv/tvurceVysledku	Cabal, J. Kohout, Michal Liška, František Pícha, Jan Kivala, Milan Kuča, K.
http://linked.open...n/vavai/riv/zamer	http://linked.opendata.cz/resource/domain/vavai/zamer/MSM%20223100001
issn	1475-6366
number of pages	5 (xsd:int)
http://localhost/t...ganizacniJednotka	22310
is http://linked.open...avai/riv/vysledek of	A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents

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