engleski

Imidazole derivatives. Bis-imidazolium and imidazolium-pyridinium oximes: reaction, inhibition and protective action on soman phosphylated human erythrocyte acetylcholinesterase. VII.

The inhibitory power (IC50), reactivation of soman phosphylated AChE and protection of human erythrocyte AchE against inhibition by soman, were detrmined by applying bis-imidazolium and two pyridinium-imidazolium oximes containing methyl, benzyl, phenyl and 4-fluorophenyl substituents at position 3 of the imidazole ring. The rings were linked with alkylidene, ether and diether chains. The IC-50 values varied from 2x10-8 to 2x10-4 mol/L. The oximes with six C-atoms in the alkylidene chain, except 2B with four C-atoms, showed the highest inhibitory power of all investigated compounds. The type of substituent on the imidazole ring and the length of the chain between rings have a significant influence on the IC-50 of these oximes. It seems that newly synthesized bis- imidazolium oximes are stronger inhibitors than pyridinium-imidazolium compounds. Only compound 2B from the oximes tested is a week inhibitor, has good reactivation potency and protective ability for AchE inhibited by soman. All the other oximes tested have not these properties which can be explained by their strong inhibitory power.

Imidazolium-pyridinium oximes ; acetylcholinesterase

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