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Tacroximes: novel unique compounds for the recovery of organophosphorus-inhibited acetylcholinesterase.

Lukas GoreckiLucie JunovaTomas KuceraVendula HepnarovaLukas PrchalTereza KobrlovaLubica MúčkováOndrej SoukupJan Korabecny
Published in: Future medicinal chemistry (2019)
Aim: Organophosphorus compounds are irreversible inhibitors of AChE. Without immediate countermeasure, intoxication leads quickly to death. None of the clinically-used causal antidotes can ensure a good prognosis for any poisoned patient. When fallen into the wrong hands, organophosphates represent a serious threat to mankind. Results & methodology: Herein, we describe two novel compounds as unique merged molecules built on a tacrine scaffold against organophosphorus intoxication. These reactivators of AChE have balanced physicochemical properties, and should be able to cross the blood-brain barrier with a slightly lowered cytotoxicity profile compared to reference tacrine. Conclusion: Their efficiency compared with pralidoxime and obidoxime was proved against dichlorvos.
Keyphrases
  • case report
  • tissue engineering