| Title : Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase - Mercey_2012_J.Med.Chem_55_10791 |
| Author(s) : Mercey G , Renou J , Verdelet T , Kliachyna M , Baati R , Gillon E , Arboleas M , Loiodice M , Nachon F , Jean L , Renard PY |
| Ref : Journal of Medicinal Chemistry , 55 :10791 , 2012 |
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Abstract :
Pyridinium and bis-pyridinium aldoximes are used as antidotes to reactivate acetylcholinesterase (AChE) inhibited by organophosphorus nerve agents. Herein, we described a series of nine nonquaternary phenyltetrahydroisoquinoline-pyridinaldoxime conjugates more efficient than or as efficient as pyridinium oximes to reactivate VX-, tabun- and ethyl paraoxon-inhibited human AChE. This study explores the structure-activity relationships of this new family of reactivators and shows that 1b-d are uncharged hAChE reactivators with a broad spectrum. |
| PubMedSearch : Mercey_2012_J.Med.Chem_55_10791 |
| PubMedID: 23148598 |
Mercey G, Renou J, Verdelet T, Kliachyna M, Baati R, Gillon E, Arboleas M, Loiodice M, Nachon F, Jean L, Renard PY (2012)
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase
Journal of Medicinal Chemistry
55 :10791
Mercey G, Renou J, Verdelet T, Kliachyna M, Baati R, Gillon E, Arboleas M, Loiodice M, Nachon F, Jean L, Renard PY (2012)
Journal of Medicinal Chemistry
55 :10791