About: Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies

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About: Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	New series of twenty six monooxime-monocarbamoyl xylene linked bispyridinium compounds was prepared. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime, K107, K108 and K203) and the prepared compounds were tested in vitro on a model of tabun- and paraoxon-, methylparaoxon- and DFP-inhibited human erythrocyte acetylcholinesterase. Although their reactivation ability against tabun did not exceed the previously known compounds, some newly prepared compounds showed promising ability in reactivation of pesticide-inhibited AChE. The acute toxicity of the novel compounds was determined. The docking study for tabun-inhibited AChE was performed for 3 compounds of interest. The structure-activity relationship (SAR) study confirmed apparent influence of xylene linkage and carbamoyl moiety on the reactivation ability and toxicity. New series of twenty six monooxime-monocarbamoyl xylene linked bispyridinium compounds was prepared. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime, K107, K108 and K203) and the prepared compounds were tested in vitro on a model of tabun- and paraoxon-, methylparaoxon- and DFP-inhibited human erythrocyte acetylcholinesterase. Although their reactivation ability against tabun did not exceed the previously known compounds, some newly prepared compounds showed promising ability in reactivation of pesticide-inhibited AChE. The acute toxicity of the novel compounds was determined. The docking study for tabun-inhibited AChE was performed for 3 compounds of interest. The structure-activity relationship (SAR) study confirmed apparent influence of xylene linkage and carbamoyl moiety on the reactivation ability and toxicity. (en)
Title	Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies (en)
skos:prefLabel	Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies Monooxime-monocarbamoyl bispyridinium xylene linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies (en)
skos:notation	RIV/60162694:G44__/10:00002295!RIV11-MO0-G44_____
http://linked.open...avai/riv/aktivita	S Z
http://linked.open...avai/riv/aktivity	S, Z(MO0FVZ0000501), Z(MSM0021620822)
http://linked.open...iv/cisloPeriodika	2
http://linked.open...vai/riv/dodaniDat	2011
http://linked.open...aciTvurceVysledku	Novotný, Ladislav Misík, Jan Kuča, Kamil Musílek, Kamil Pohanka, Doc. RNDr. PhD, Miroslav
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	272567
http://linked.open...ai/riv/idVysledku	RIV/60162694:G44__/10:00002295
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	acetylcholinesterase; organophosphate; reactivator; tabun; pesticide; xylene linker; docking (en)
http://linked.open.../riv/klicoveSlovo	xylene linker organophosphate docking pesticide acetylcholinesterase tabun reactivator
http://linked.open...odStatuVydavatele	DE - Spolková republika Německo
http://linked.open...ontrolniKodProRIV	[0980CB431D44]
http://linked.open...i/riv/nazevZdroje	ChemMedChem
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	5 (xsd:int)
http://linked.open...cetTvurcuVysledku	8 (xsd:int)
http://linked.open...UplatneniVysledku	2010
http://linked.open...v/svazekPeriodika	5
http://linked.open...iv/tvurceVysledku	Dohnal, Vlastimil Kuča, Kamil Misík, Jan Musílek, Kamil Novotný, Ladislav Pohanka, Miroslav Opletalová, Veronika Holas, Ondřej
http://linked.open...ain/vavai/riv/wos	000274538600009
http://linked.open...n/vavai/riv/zamer	Zdravotnická problematika ZHN Research of new drug structures
issn	1860-7179
number of pages	8 (xsd:int)
http://localhost/t...ganizacniJednotka	G44

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