Reactivation study of pyridinium oximes for acetylcholinesterases inhibited by paraoxon or DFP

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Novel bisquaternary oximes--reactivation of acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon.

Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, their biological activity was evaluated for their ability to reactivate acetylcholinesterase (AChE; EC 3.1.1.7) and butyrylcholinesterase (BuChE; EC 3.1.1.8) inhibited by paraoxon. Their reactivation activity was compared with standard reactivators--pralidoxime, obidoxi...

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An in vitro comparative study on the reactivation of nerve agent-inhibited guinea pig and human acetylcholinesterases by oximes.

The reactivation of nerve agent-inhibited acetylcholinesterase (AChE) by oxime is the most important step in the treatment of nerve agent poisoning. Since the evaluation of nerve agent antidotes cannot be conducted in humans, results from animal experiments are extrapolated to humans. Guinea pig is one of the animal models that is frequently used for conducting nerve agent antidote evaluations....

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The Length Dependent Activity of Oximes on Reactivation of Tabun Inhibited Acetylcholinesterase; A Theoretical Study

In this work, the effect of ligand's length on interaction energy of six oximes, A [2-(hydroxyimino)-N-((1-(2-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)ethyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide], B [2-(hydroxyimino)-N-((1-(3-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)propyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide], C [2-(hydroxyimino)-N-((1-(4-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)but...

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the length dependent activity of oximes on reactivation of tabun inhibited acetylcholinesterase; a theoretical study

in this work, the effect of ligand's length on interaction energy of six oximes, a [2-(hydroxyimino)-n-((1-(2-(2-((hydroxyimino)methyl)-1h-imidazol-1-yl)ethyl)-1h-1,2,3-triazol-4-yl)methyl)acetamide], b [2-(hydroxyimino)-n-((1-(3-(2-((hydroxyimino)methyl)-1h-imidazol-1-yl)propyl)-1h-1,2,3-triazol-4-yl)methyl)acetamide], c [2-(hydroxyimino)-n-((1-(4-(2-((hydroxyimino)methyl)-1h-imidazol-1-y...

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The kinetics of reactivation, by oximes, of cholinesterase inhibited by organophosphorus compounds.

The inhibition of cholinesterase (ChE) and related enzymes, by organophosphorus compounds, is generally believed to occur by direct phosphorylation of some group at the active centre of the enzyme, together with the liberation of an acid anion (Wilson, 1951; Balls & Jansen, 1952; Hartley & Kilby, 1952; Aldridge, 1954; Kilby & Youatt, 1954). Inhibition by organophosphorus compounds is generally ...

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ژورنال

عنوان ژورنال: Journal of Applied Biomedicine

سال: 2006

ISSN: 1214-021X,1214-0287

DOI: 10.32725/jab.2006.006