What is it about?

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).

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Why is it important?

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).

Perspectives

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).

Dr Vladimír Církva
Institute of Chemical Process Fundamentals

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This page is a summary of: Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases, Letters in Drug Design & Discovery, May 2010, Elsevier,
DOI: 10.2174/157018010790945823.
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