engleski

Novel heterocyclic oximes and their interactions with butirylcholinesterases

Highly toxic acetylcholinesterase inhibiting pesticides, organophosphates (OP) and carbamates are intensively used troughout the world and continue to be responsible for poisoning and deaths.1, 2 Since there is still no single, broad-spectrum compound suitable for the antidotal treatment of poisoning with all OP agents a series of novel aliphatic and aromatic quaternary salts of N-alkyl/aryl imidazol- and benzimidazole-2-aldoximes have been prepared as potential reactivators of inhibited butyrylcholinesterase. N-alkylations were carried out with the appropriate electrophile in 50% aqeous NaOH and small amount of DMSO to assure better dissolving for reagents. N-alkyl/aryl azoles were converted to the appropriate 2-carbaldehydes by using modified Ivesen-Lund method3 and then to 2- aldoximes. Reaction with the alkyl/aryl halogenides resulted in a desired quaternary salts. Inhibitory properties of prepared compounds and their reactivation efficiency of Paraoxon inhibited human butyrylcholinesterase as well as horse, rabbit and guinea pig serum will be tested. Structural characteristics of an efficient oxime reactivator will be discussed.

imidazole ; benzimidazole ; cholinesterase

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