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Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase

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Kliachyna, Maria | Santoni, Gianluca | Nussbaum, Valentin | Renou, Julien | Sanson, Benoît | Colletier, Jacques-Philippe | Arboléas, Mélanie | Loiodice, Mélanie | Weik, Martin | Jean, Ludovic | Renard, Pierre-Yves | Nachon, Florian | Baati, Rachid

Edité par CCSD ; Elsevier -

International audience. A series of new uncharged functional acetylcholinesterase (AChE) reactivators including heterodimers of tetrahydroacridine with 3-hydroxy-2-pyridine aldoximes and amidoximes has been synthesized. These novel molecules display in vitro reactivation potencies towards VX-, tabun- and paraoxon-inhibited human AChE that are superior to those of the mono- and bis-pyridinium aldoximes currently used against nerve agent and pesticide poisoning. Furthermore, these uncharged compounds exhibit a broader reactivity spectrum compared to currently approved remediation drugs.

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