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

Publikace |
2019

Tento text není v aktuálním jazyce dostupný. Zobrazuje se verze "en".Abstrakt

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. [GRAPHICS] .