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