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Description
| - The reactivators of acetylcholinesterase are very important components in the treatment of intoxications caused by organophosphate inhibitors such as tabun, sarin, soman, VX etc. and insecticides like echothiofat, metrifonat, chlorpyrifos etc. These inhibitors covalently bind on active site of mentioned enzyme and irreversibly inhibit its activity. The reactivator breaks the inhibitor-enzyme covalent bond and restores its activity. Unfortunately, there is no reactivator applicable for every type of inhibition; it means that every structural change in the molecule of inhibitor needs a specific structure of the reactivator. Therefore, development of more active acetylcholinesterase reactivators with broader spectrum is a major challenge actual from the point of view of war operations, accidents or terroristic attacks. Synthetic approaches, biological activity evaluation and structure-activity relationship studies of newly prepared acetylcholinesterase reactivators from 1990 to 2004 are summarized. Synth
- The reactivators of acetylcholinesterase are very important components in the treatment of intoxications caused by organophosphate inhibitors such as tabun, sarin, soman, VX etc. and insecticides like echothiofat, metrifonat, chlorpyrifos etc. These inhibitors covalently bind on active site of mentioned enzyme and irreversibly inhibit its activity. The reactivator breaks the inhibitor-enzyme covalent bond and restores its activity. Unfortunately, there is no reactivator applicable for every type of inhibition; it means that every structural change in the molecule of inhibitor needs a specific structure of the reactivator. Therefore, development of more active acetylcholinesterase reactivators with broader spectrum is a major challenge actual from the point of view of war operations, accidents or terroristic attacks. Synthetic approaches, biological activity evaluation and structure-activity relationship studies of newly prepared acetylcholinesterase reactivators from 1990 to 2004 are summarized. Synth (en)
- Reaktivátory acetylcholinesterasy jsou velmi důležitou součástí léčby intoxikací způsobených organofosforovými inhibitory jako např. tabunem, sarinem, somanem, látkou VX a insekticidy jako např. echothiofátem, metrifonátem nebo chlorpyrifosem. Tyto inhibitory se kovalentně váží na aktivní místo enzymu a ireverzibilně inhibují jeho aktivitu. Reaktivátor štěpí kovalentní vazbu enzym-inhibitor a obnovuje aktivitu enzymu. Žádný z reaktivátorů není použitelný pro všechny typy inhibice, protože každá změna ve struktuře molekuly inhibitoru vyžaduje specifickou strukturu reaktivátoru. Vývoj více aktivních a širokospektrých reaktivátorů je proto aktuální z pohledu válečným operací, nehod nebo teroristických útoků. Pokroky v syntéze sloučenin, jejich testování a vztahy mezi strukturou a aktivitou zpracovány pro období 1990-2004. Použité syntetické postupy a testovací metody jsou zaznamenány pro jednotlivé typy reaktivátorů. Důraz byl kladen zejména na deriváty pyridinkarbaldoximu a imidazolkarbaldoximu. (cs)
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Title
| - Progress in synthesis of new acetylcholinesterase reactivators in period 1990-2004
- Progress in synthesis of new acetylcholinesterase reactivators in period 1990-2004 (en)
- Pokroky v syntéze nových reaktivátorů acetylcholinesterasy v letech 1990-2004 (cs)
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skos:prefLabel
| - Progress in synthesis of new acetylcholinesterase reactivators in period 1990-2004
- Progress in synthesis of new acetylcholinesterase reactivators in period 1990-2004 (en)
- Pokroky v syntéze nových reaktivátorů acetylcholinesterasy v letech 1990-2004 (cs)
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skos:notation
| - RIV/60162694:G44__/07:00001764!RIV08-MO0-G44_____
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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
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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/60162694:G44__/07:00001764
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - acetylcholinesterase reactivators (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - AE - Stát Spojené arabské emiráty
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Current Organic 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
| - Doležal, Martin
- Kuča, Kamil
- Musílek, Kamil
- Jun, Daniel
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issn
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number of pages
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http://localhost/t...ganizacniJednotka
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