Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon

Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, their biological activity was evaluated for their ability to reactivate acetylcholinesterase (AChE; EC 3.1.1.7) and butyryl-cholinesterase (BuChE; EC 3.1.1.8) inhibited by p...

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Autores principales: Kuca, Kamil, Musilova, Lucie, Palecek, Jiri, Cirkva, Vladimir, Paar, Martin, Musilek, Kamil, Hrabinova, Martina, Pohanka, Miroslav, Karasova, Jana Zdarova, Jun, Daniel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International 2009
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6255039/
https://www.ncbi.nlm.nih.gov/pubmed/20032868
http://dx.doi.org/10.3390/molecules14124915
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author Kuca, Kamil
Musilova, Lucie
Palecek, Jiri
Cirkva, Vladimir
Paar, Martin
Musilek, Kamil
Hrabinova, Martina
Pohanka, Miroslav
Karasova, Jana Zdarova
Jun, Daniel
author_facet Kuca, Kamil
Musilova, Lucie
Palecek, Jiri
Cirkva, Vladimir
Paar, Martin
Musilek, Kamil
Hrabinova, Martina
Pohanka, Miroslav
Karasova, Jana Zdarova
Jun, Daniel
author_sort Kuca, Kamil
collection PubMed
description Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, their biological activity was evaluated for their ability to reactivate acetylcholinesterase (AChE; EC 3.1.1.7) and butyryl-cholinesterase (BuChE; EC 3.1.1.8) inhibited by paraoxon. Their reactivation activity was compared with standard reactivators—pralidoxime, obidoxime and HI-6—which are clinically used at present. As it resulted, none of the prepared compounds surpassed obidoxime, which is considered to be the most potent compound if used for reactivation of AChE inhibited by paraoxon. In case of BuChE reactivation, two compounds (K053 and K068) achieved similar results as obidoxime.
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spelling pubmed-62550392018-11-30 Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon Kuca, Kamil Musilova, Lucie Palecek, Jiri Cirkva, Vladimir Paar, Martin Musilek, Kamil Hrabinova, Martina Pohanka, Miroslav Karasova, Jana Zdarova Jun, Daniel Molecules Article Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, their biological activity was evaluated for their ability to reactivate acetylcholinesterase (AChE; EC 3.1.1.7) and butyryl-cholinesterase (BuChE; EC 3.1.1.8) inhibited by paraoxon. Their reactivation activity was compared with standard reactivators—pralidoxime, obidoxime and HI-6—which are clinically used at present. As it resulted, none of the prepared compounds surpassed obidoxime, which is considered to be the most potent compound if used for reactivation of AChE inhibited by paraoxon. In case of BuChE reactivation, two compounds (K053 and K068) achieved similar results as obidoxime. Molecular Diversity Preservation International 2009-12-01 /pmc/articles/PMC6255039/ /pubmed/20032868 http://dx.doi.org/10.3390/molecules14124915 Text en © 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Kuca, Kamil
Musilova, Lucie
Palecek, Jiri
Cirkva, Vladimir
Paar, Martin
Musilek, Kamil
Hrabinova, Martina
Pohanka, Miroslav
Karasova, Jana Zdarova
Jun, Daniel
Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon
title Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon
title_full Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon
title_fullStr Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon
title_full_unstemmed Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon
title_short Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon
title_sort novel bisquaternary oximes—reactivation of acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6255039/
https://www.ncbi.nlm.nih.gov/pubmed/20032868
http://dx.doi.org/10.3390/molecules14124915
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