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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Kamil Kuca

Volume 7, Issue 4, 2010

Page: [260 - 264] Pages: 5

DOI: 10.2174/157018010790945823

Price: $65

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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