engleski

Quinuclidinium derivatives as inhibitors of cholinesterases, reactivators of the phosphorylated enzymes and antidotes against poisoning by organophosphates

Many quinuclidinium derivatives have been recognized as pharmaceutical agents and several were tested in the therapy of animals poisoned by organophosphorus compounds. Thirteen quinuclidinium derivatives were prepared in Croatia over the past seven years meant for testing their interaction with cholinesterases as well as their antidotal potency in poisoning of animals by organophosphorus compounds. They are quaternized monoquinuclidinium derivatives or their conjugates with another quaternized quinuclidinium, pyridinium or imidazolium ring. Three compounds have two oxime groups, seven are monooximes and three compounds do not bear an oxime group. The compounds were analyzed in their reaction with acetylcholinesterase in vitro and in their antidotal impact in vivo against poisoning by soman and tabun. The properties of the compounds concerning the above parameters were compared with those of the four standard oximes PAM-2, Toxogonin, HI-6 and TMB-4.

quinuclidinium compounds; oximes; antidotes; soman; tabun; protection; reactivation; therapy

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