| Title : Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase - Kliachyna_2014_Eur.J.Med.Chem_78C_455 |
| Author(s) : Kliachyna M , Santoni G , Nussbaum V , Renou J , Sanson B , Colletier JP , Arboleas M , Loiodice M , Weik M , Jean L , Renard PY , Nachon F , Baati R |
| Ref : Eur Journal of Medicinal Chemistry , 78C :455 , 2014 |
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Abstract :
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. |
| PubMedSearch : Kliachyna_2014_Eur.J.Med.Chem_78C_455 |
| PubMedID: 24704618 |
| Inhibitor | Tacrine-pyridinealdoxime-1 |
| Reactivator | Tacrine-pyridinealdoxime-1 Tacrine-pyridinealdoxime-2 |
Kliachyna M, Santoni G, Nussbaum V, Renou J, Sanson B, Colletier JP, Arboleas M, Loiodice M, Weik M, Jean L, Renard PY, Nachon F, Baati R (2014)
Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase
Eur Journal of Medicinal Chemistry
78C :455
Kliachyna M, Santoni G, Nussbaum V, Renou J, Sanson B, Colletier JP, Arboleas M, Loiodice M, Weik M, Jean L, Renard PY, Nachon F, Baati R (2014)
Eur Journal of Medicinal Chemistry
78C :455