Casualties caused by nerve agents, potent acetylcholinesterase inhibitors, have attracted attention from media recently. Poisoning with these chemicals may be fatal if not correctly addressed. Therefore, research on novel antidotes is clearly warranted. Pyridinium oximes are the only clinically available compounds, but poor penetration into the blood-brain barrier hampers efficient enzyme reactivation at the central nervous system. In searching for structural factors that may be explored in SAR studies, we synthesized and evaluated neutral aryloximes as reactivators for acetylcholinesterase inhibited by NEMP, a VX surrogate. Although few tested compounds reached comparable reactivation results with clinical standards, they may be considered as leads for further optimization.
Cavalcante SFA, Kitagawa DAS, Rodrigues RB, Bernardo LB, da Silva TN, Dos Santos WV, Correa ABA, de Almeida JSFD, Franca TCC, Kuca K, Simas ABC (2019) Synthesis and in vitro evaluation of neutral aryloximes as reactivators of Electrophorus eel acetylcholinesterase inhibited by NEMP, a VX surrogate Chemico-Biological Interactions309: 108682
Cavalcante SFA, Kitagawa DAS, Rodrigues RB, Bernardo LB, da Silva TN, Dos Santos WV, Correa ABA, de Almeida JSFD, Franca TCC, Kuca K, Simas ABC (2019) Chemico-Biological Interactions309: 108682
