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Title: Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase. Author: Kliachyna M, Santoni G, Nussbaum V, Renou J, Sanson B, Colletier JP, Arboléas M, Loiodice M, Weik M, Jean L, Renard PY, Nachon F, Baati R. Journal: Eur J Med Chem; 2014 May 06; 78():455-67. PubMed ID: 24704618. 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.[Abstract] [Full Text] [Related] [New Search]