About: Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase

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About: Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Eighteen monoquaternary reactivators of acetylcholinesterase with modified side chain were developed in an effort to extend the properties of pralidoxime. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) and the prepared compounds were tested in vitro on a model of tabun and paraoxon-inhibited AChE. Monoquaternary reactivators were not able to exceed the best known compounds for tabun poisoning, but some of them did show reactivation better or comparable with pralidoxime for paraoxon poisoning. However, extensive differences were found by a SAR study for various side chains on the non-oxime part of the reactivator molecule. Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Eighteen monoquaternary reactivators of acetylcholinesterase with modified side chain were developed in an effort to extend the properties of pralidoxime. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) and the prepared compounds were tested in vitro on a model of tabun and paraoxon-inhibited AChE. Monoquaternary reactivators were not able to exceed the best known compounds for tabun poisoning, but some of them did show reactivation better or comparable with pralidoxime for paraoxon poisoning. However, extensive differences were found by a SAR study for various side chains on the non-oxime part of the reactivator molecule. (en) Bylo připraveno osmnáct monokvarterních sloučenin s modifikovaných bočním řetězcem, které byly testovány proti tabunem a paraoxonem inhibované acetylcholinesterase. (cs)
Title	Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase (en) Monokvarterní pyridiniové soli s modifikovaných bočním řetězcem - syntéza a evaluace na modelu acetylcholinesterasy inhibované tabunem a paraoxonem (cs)
skos:prefLabel	Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase (en) Monokvarterní pyridiniové soli s modifikovaných bočním řetězcem - syntéza a evaluace na modelu acetylcholinesterasy inhibované tabunem a paraoxonem (cs)
skos:notation	RIV/60162694:G44__/08:00002002!RIV09-MSM-G44_____
http://linked.open...avai/riv/aktivita	P S
http://linked.open...avai/riv/aktivity	P(ME 865), S
http://linked.open...iv/cisloPeriodika	17
http://linked.open...vai/riv/dodaniDat	2009
http://linked.open...aciTvurceVysledku	Jun, Daniel Kuča, Kamil Musílek, 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	Ministerstvo obrany / Univerzita obrany - Fakulta vojenského zdravotnictví Hradec Králové
http://linked.open...dnocenehoVysledku	380556
http://linked.open...ai/riv/idVysledku	RIV/60162694:G44__/08:00002002
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	acetylcholinesterase; tabun; paraoxon; reactivator; oxime; monoquaternary (en)
http://linked.open.../riv/klicoveSlovo	acetylcholinesterase tabun paraoxon oxime reactivator monoquaternary
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[CC5AB7A1B941]
http://linked.open...i/riv/nazevZdroje	Bioorganic & Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	FP
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	6 (xsd:int)
http://linked.open...vavai/riv/projekt	http://linked.opendata.cz/resource/domain/vavai/projekt/ME%20865
http://linked.open...UplatneniVysledku	2008
http://linked.open...v/svazekPeriodika	16
http://linked.open...iv/tvurceVysledku	Dohnal, Vlastimil Kuča, Kamil Musílek, Kamil Kučera, Jiří Jun, Daniel Opletalová, Veronika
http://linked.open...ain/vavai/riv/wos	000258827800041
issn	0968-0896
number of pages	6 (xsd:int)
http://localhost/t...ganizacniJednotka	G44

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