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rdf:type
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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)
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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)
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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)
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skos:notation
| - RIV/60461373:22310/05:00013840!RIV06-MSM-22310___
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http://linked.open.../vavai/riv/strany
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
| - P(GA203/01/1093), Z(MSM 223100001)
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/60461373:22310/05:00013840
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - Acetylcholinesterase; Reactivator; PNPA; Reactivation; Verve agents; Inhibition (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - GB - Spojené království Velké Británie a Severního Irska
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Journal of Enzyme Inhibition and Medicinal Chemistry
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Cabal, J.
- Kohout, Michal
- Liška, František
- Pícha, Jan
- Kivala, Milan
- Kuča, K.
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http://linked.open...n/vavai/riv/zamer
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issn
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number of pages
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http://localhost/t...ganizacniJednotka
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is http://linked.open...avai/riv/vysledek
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