| Literature DB >> 31163137 |
Samir F de A Cavalcante1, Daniel A S Kitagawa2, Rafael B Rodrigues3, Leandro B Bernardo3, Thiago N da Silva4, Wellington V Dos Santos5, Ana Beatriz de A Correa3, Joyce S F D de Almeida2, Tanos C C França6, Kamil Kuča7, Alessandro B C Simas8.
Abstract
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.Entities:
Keywords: Acetylcholinesterase reactivators; Chemical defence; Drug screening; Nerve agents' surrogates; Neutral oximes
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Year: 2019 PMID: 31163137 DOI: 10.1016/j.cbi.2019.05.048
Source DB: PubMed Journal: Chem Biol Interact ISSN: 0009-2797 Impact factor: 5.192