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Molecules 2009, 14(12), 4915-4921; doi:10.3390/molecules14124915

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

1
Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic
2
Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Hradec Kralove, Czech Republic
3
Institut für Organische Chemie and Zentrum für Biomolekulare Wirkstoffe (BMWZ), Leibniz Universität Hannover, Hannover, Germany
4
Institute of Chemical Process Fundamentals of the ASCR, v. v. i., Prague, Czech Republic
5
Faculty of Environmental Sciences, Czech University of Life Sciences Prague, Praha, Czech Republic
*
Author to whom correspondence should be addressed.
Received: 26 October 2009 / Revised: 24 November 2009 / Accepted: 27 November 2009 / Published: 1 December 2009
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Abstract

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 butyrylcholinesterase (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.
Keywords: acetylcholinesterase; butyrylcholinesterase; reactivator; nerve agent; oxime; pesticide; scavenger acetylcholinesterase; butyrylcholinesterase; reactivator; nerve agent; oxime; pesticide; scavenger
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Kuca, K.; Musilova, L.; Palecek, J.; Cirkva, V.; Paar, M.; Musilek, K.; Hrabinova, M.; Pohanka, M.; Karasova, J.Z.; Jun, D. Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon. Molecules 2009, 14, 4915-4921.

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