About: Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun - and paraoxon-inhibited acetylcholinesterase

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About: Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against 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	Six AChE monooxime-monocarbamoyl reactivators with an (E)-but-2-ene linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and insecticide paraoxon was tested in vitro. The reactivation efficacies of pralidoxime, HI-6, obidoxime, K048, K075 and the newly prepared reactivators were compared. According to the results obtained, one reactivator seems to be promising against tabun-inhibited AChE and two reactivators against paraoxon-inhibited AChE. The best results were obtained for bisquaternary substances with at least one oxime group in position four. Six AChE monooxime-monocarbamoyl reactivators with an (E)-but-2-ene linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and insecticide paraoxon was tested in vitro. The reactivation efficacies of pralidoxime, HI-6, obidoxime, K048, K075 and the newly prepared reactivators were compared. According to the results obtained, one reactivator seems to be promising against tabun-inhibited AChE and two reactivators against paraoxon-inhibited AChE. The best results were obtained for bisquaternary substances with at least one oxime group in position four. (en) Bylo připraveno šest monooximových-monokarbamoylovaných bispyridiniových sloučenin nesoucích (E)-but-2-enový spojovací řetězec, které byly testovány proti tabunem a paraoxonem inhibované acetylcholinesterase. (cs)
Title	Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun - and paraoxon-inhibited acetylcholinesterase Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun - and paraoxon-inhibited acetylcholinesterase (en) Syntéza monooximových-monokarbamoylovaných bispyridiniových sloučenin nesoucích (E)-but-2-enový spojovací řetězec a jejich evaluace proti tabunem a paraoxonem inhibované acetylcholinesterase (cs)
skos:prefLabel	Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun - and paraoxon-inhibited acetylcholinesterase Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun - and paraoxon-inhibited acetylcholinesterase (en) Syntéza monooximových-monokarbamoylovaných bispyridiniových sloučenin nesoucích (E)-but-2-enový spojovací řetězec a jejich evaluace proti tabunem a paraoxonem inhibované acetylcholinesterase (cs)
skos:notation	RIV/60162694:G44__/08:00002000!RIV09-MO0-G44_____
http://linked.open...avai/riv/aktivita	S Z
http://linked.open...avai/riv/aktivity	S, Z(MO0FVZ0000501)
http://linked.open...iv/cisloPeriodika	1
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	398785
http://linked.open...ai/riv/idVysledku	RIV/60162694:G44__/08:00002000
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	acetylcholinesterase; reactivation; nerve agent; tabun; pesticide; paraoxon; reactivator; oxime; inhibition (en)
http://linked.open.../riv/klicoveSlovo	inhibition pesticide acetylcholinesterase reactivation tabun paraoxon nerve agent oxime reactivator
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[351BF517AA70]
http://linked.open...i/riv/nazevZdroje	Journal of Enzyme Inhibition and Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	FP
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...UplatneniVysledku	2008
http://linked.open...v/svazekPeriodika	23
http://linked.open...iv/tvurceVysledku	Doležal, Martin Dohnal, Vlastimil Kuča, Kamil Musílek, Kamil Jun, Daniel Opletalová, Veronika Holas, Ondrej
http://linked.open...ain/vavai/riv/wos	000253122700012
http://linked.open...n/vavai/riv/zamer	Zdravotnická problematika ZHN
issn	1475-6366
number of pages	7 (xsd:int)
http://localhost/t...ganizacniJednotka	G44

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