Pavlikova_2010_Mil.Med.Sci.Lett_79_46

The prophylactic antidotes are pharmaceutics which can prevent the intoxication of the human body or may improve its prognosis if administered before the exposure to a toxic substance. Pyridostigmine chloride, a reversible acetylcholinesterase(AChE) inhibitor, is used as a prophylactic antidote which may prevent the organism from organophosphorus poisoning (OP). This paper is focused on searching new AChE inhibitors that might be used in prophylactic treatment of OP intoxications. The aim of this study was to prepare 15 symmetric bisquaternary inhibitors and to evaluate their inhibition ability (IC50) via a standard in vitro method. The but-(2E)-en-1,4-diyl-1,1'-bis(4-(4-nitrobenzyl)-pyridinium) dibromide was selected, on the basis of IC50 value, the most potent AChE inhibitor.