Chapter 16: Synthesis of New Reactivators of Cholinesterase.

Autor: Petrova, Iskra, Samnaliev, Ivan, Dishovsky, Christophor
Předmět:
Zdroj: Journal of Medical Chemical, Biological & Radiological Defense; 2010, Vol. 8, p115-120, 6p, 3 Diagrams
Abstrakt: Irrespective of the fact that the main mechanism of toxicity of the nerve agents (tabun, sarin, soman, cyclosarin, VX) - inhibition of acetylcholinesterse (AChE) in peripheral and central nervous systems is very well known there are some unresolved problems related to the antidote treatment of this type of poisoning. One of the most important question is that many studies have shown that none of the currently available reactivators of cholinesterase, such as 2-PAM, obidoxime (toxogonin), HI-6 and trimedoxime is able to reactivate AChE inhibited by all compounds belonging to the nerve agents. That is way a lot of new cholinesterase reactvators with different chemical structure have been synthesized and tested by using in vitro or in vivo methods for their antidote activity. In our study we describe the synthesis of some new reacrivators of ChE and the results obtained for their therapeutic efficacy in rats poisoned with soman and tabun. Our date have shown that two of compounds - BT-05 and BT-07 4M combined with atropine demonstrated very good effectiveness against tabun. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index