Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases

Author(s): Lucie Musilova, Daniel Jun, Jiri Palecek, Vladimir Cirkva, Kamil Musilek, Martin Paar, Martina Hrabinova, Miroslav Pohanka, Kamil Kuca.

Abstract:

New cholinesterase reactivators are synthesized as potential antidotes for treatment of organophosphorus agent poisonings or as part of pseudo catalytic scavengers for improvement of the nerve agent prophylaxis. In this study, three novel potential cholinesterase reactivators (K064 - (E)-1-(pyridinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K065-(E)-1-(quinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K066-(E)-1- (isoquinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide) were synthesized and tested for their potency to reactivate acetylcholinesterase (AChE, EC 3.1.1.3) and butyrylcholinesterase (BChE, 3.1.1.8) inhibited by pesticide paraoxon. As resulted, none from the synthesized compounds surpassed currently clinically used reactivators (pralidoxime, obidoxime and HI-6).

Keywords: Acetylcholinesterase, Butyrylcholinesterase, Nerve agent, Pesticide, Reactivator, Oxime, Paraoxon, Scavenger

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Article Details

VOLUME: 7
ISSUE: 4
Year: 2010
Page: [260 - 264]
Pages: 5
DOI: 10.2174/157018010790945823
Price: $58