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- W2944491115 abstract "Toxic organophosphorus compounds inhibit acetylcholinesterase (AChE; EC 3.1.1.7) in the synapses of the peripheral and central nervous system (CNS) and cause death or long-term neurological impairments. Therapy includes oxime reactivators of the inhibited AChE, but they do not achieve sufficient concentrations in the CNS. The efficiency of newly-synthesized hydroxyl-pyridine and chloro-pyridinium oximes, designed with an aim to cross into the CNS, was evaluated here with a detailed kinetic investigation of the reactivation of AChE and butyrylcholinesterase (EC 3.1.1.8) inhibited by sarin, cyclosarin, VX, tabun and paraoxon. Analyses of physicochemical properties important for crossing into the CNS, in vitro toxicity, metabolic stability and pharmacokinetic profile in mouse model, were used for the rational determination of the lead oxime for further tests, 2-((hydroxyimino)methyl)-6-(4-(morpholin-4-yl)butyl)pyridin-3-ol oxime, that has potency to reactivate AChE in peripheral tissues and the brain. This approach enabled better screening for lead compounds in comparison to the standard analysis based on the reactivation efficiency of the oximes. Therefore, this kind of reactivatior evaluation is recommended before in vivo antidotal testing, as it would singificantly improve adherence to rules for animal welfare." @default.
- W2944491115 created "2019-05-16" @default.
- W2944491115 creator A5062391042 @default.
- W2944491115 date "2019-11-09" @default.
- W2944491115 modified "2023-09-28" @default.
- W2944491115 title "Novi pristup analizi oksima dizajniranih za zaštitu središnjeg živčanog sustava pri trovanju organofosfornim spojevima" @default.
- W2944491115 hasPublicationYear "2019" @default.
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