Karasova_2010_Mil.Med.Sci.Lett_79_23

The penetration of acetylcholinesterase (AChE) reactivators through the blood-brain barrier is hotly discussed question nowadays. The increase of lipophilicity of these compounds is one of the possible ways how to increase their penetration and also their efficacy in the central nervous system.The aim of this study is to compare the reactivation potency of newly synthesized oxime - oxime K203 - after its fluorination. This AChE reactivator was prepared at the Research Institute of Chemical Technology (Korea) and is known as K22836. The fluorination of oxime K203 leads to reduction of its therapeutic efficacy. The reactivation potency of newly synthesized oxime K22836 was lower in the whole blood and also in the central nervous system. In summary, the most efficacious reactivator in case of tabun-inhibited AChE is still oxime K203 originally prepared at our department.