
European Journal of Medicinal Chemistry p. 455 - 467 (2014)
Update date:2022-07-30
Topics:
Kliachyna, Maria
Santoni, Gianluca
Nussbaum, Valentin
Renou, Julien
Sanson, Benoit
Colletier, Jacques-Philippe
Arboléas, Mélanie
Loiodice, Mélanie
Weik, Martin
Jean, Ludovic
Renard, Pierre-Yves
Nachon, Florian
Baati, Rachid
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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