Abstract
A family of novel efficient non-oxime compounds exhibited promising reactivation efficacy for VX and sarin inhibited human acetylcholinesterase was discovered. It was found that aromatic groups coupled to Mannich phenols and the introduction of imidazole to the ortho position of phenols would dramatically enhance reactivation efficiency. Moreover, the in vivo experiment was conducted, and the results demonstrated that Mannich phenol L10R1 (30 mg/kg, ip) could afford 100% 48 h survival for mice of 2*LD50 sarin exposure, which is promising for the development of non-oxime reactivators with central efficiency.
Highlights
Organophosphates (OPs) including pesticides and nerve agents and nerve agents are highly toxic compounds [1]
A family of novel non-oxime compounds displayed promising reactivation efficacy for VX and sarin inhibited hAChE were discovered in this paper
L6R4, L10R1, and L10R4 were proven as efficient reactivators for sarin and VX inhibited hAChE in vitro
Summary
OPs potently inhibit the cholinergic acetylFigure 1) are highly toxic compounds [1]. OPs potently inhibit the cholinergic acetylchocholinesterase (AChE) through phosphorylation of the enzyme’s catalytic serine residue, linesterase (AChE) through phosphorylation of the enzyme’s catalytic serine residue, and render it incapable of hydrolyzing the neurotransmitter acetylcholine. This inhibition and render it incapable of hydrolyzing the neurotransmitter acetylcholine. This inhibicauses accumulation of acetylcholine (ACh), and leads to cholinergic crisis, respiratory tion causes accumulation of acetylcholine (ACh), and leads to cholinergic crisis, respiradistress, convulsive seizures and and death [2]. This inhibicauses accumulation of acetylcholine (ACh), and leads to cholinergic crisis, respiratory tion causes accumulation of acetylcholine (ACh), and leads to cholinergic crisis, respiradistress, convulsive seizures and and death [2]. [2].
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