engleski

Reactivators of acetylcholinesterse inhibited by organophosphorus compounds. Imidazole derivatives. V.

This investigation was aimed at finding out to what extent the nature of the p-CH3 substituent in N-phenyl imidazolium oximes affects the in vitro inhibitory power (IC-50) on human erythrocyte AChE inhibited by soman and in vitro protection against soman. Acute toxicity (LD50)in mice, was determined in vivo as well as the protection against soman intoxication. Four new p-methylphenyl(mono-imidazolium, imidazolium-pyridinium and bis-imidazolium) oximes were prepared and characterized by elemental analysis, IR and proton NMR- spectroscopy. IC-50 values were determined only for BMR-2 and BMR-3 because BMR-1 and BMR-2 provoke <50% inhibition of human erythrocyte AChE at concentration <1x10-3 mol/L. BMR-3 was a powerful reactivator of soman inhibited hunan AChE (37%). None of the compounds offered any in vitro protection to AChE against inhibition by soman. LD50 values varied from 0.031 to 0.152 mmol/kg. Only BMR-4, given together with atropine sulfate, provided a good in vitro protection against 1.8 and 2.2 x LD50 soman.

imidazole derivatives ; acetylcholinesterase reactivation

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