Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2014

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

Maria Kliachyna
  • Fonction : Auteur
Gianluca Santoni
  • Fonction : Auteur
Valentin Nussbaum
  • Fonction : Auteur
Julien Renou
  • Fonction : Auteur
Mélanie Arboléas
  • Fonction : Auteur
Mélanie Loiodice
  • Fonction : Auteur
Ludovic Jean
Florian Nachon

Résumé

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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hal-01131268 , version 1 (13-03-2015)

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Maria Kliachyna, Gianluca Santoni, Valentin Nussbaum, Julien Renou, Benoît Sanson, et al.. Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase. European Journal of Medicinal Chemistry, 2014, 78, pp.455-467. ⟨10.1016/j.ejmech.2014.03.044⟩. ⟨hal-01131268⟩
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