A structure-activity analysis was used to evaluate the variation in oxime efficacy of 2-PAM, obidoxime, HI-6 and ICD585 against nerve agents. In vivo oxime protection and in vitro oxime reactivation were used as indicators of oxime efficacy against VX, sarin, VR and cyclosarin. Analysis of in vivo oxime protection was conducted with oxime protective ratios (PR) from guinea pigs receiving oxime ...

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...

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...

A series of oxime ether and oxime ester derivatives of the potential anti-Parkinson prodrug PD148903 (2.3) were synthesized and evaluated in pharmacological models. Oximes 4.3 (hydroxyl-oxime) and 4.4 (methoxyl-oxime) were inactive in vitro but in the Ungerstedt rat model for Parkinson’s disease 4.3 and 4.4 produced a pronounced and long lasting effect at 1.0 mg kg po. Enantiomerically pure (–)...

It has been established that oximes cause endothelium-independent relaxation in blood vessels. In the present study, the cardiovascular effects of the new oxime 3-hydroxy-4-(hydroxyimino)-2-(3-methylbut-2-enylnaphtalen-1(4H)-one (Oxime S1) derived from lapachol were evaluated. In normotensive rats, administration of Oxime S1 (10, 15, 20 and 30 mg/Kg, i.v.) produced dose-dependent reduction in b...

Indirubin, a red colored 3,2'-bisindole isomer, is a component of Indigo naturalis and is an active ingredient used in traditional Chinese medicine for the treatment of chronic diseases. The family of indirubin derivatives, such as indirubin-3'-oxime, has been suggested for various therapeutic indications. However, potential toxic interactions such as indirubin effects on mitochondrial bioenerg...

1. Reactivation of erythrocyte cholinesterase inhibited by ethyl p-nitrophenyl ethylphosphonate (armine) was studied with NN'-dimethylenebis-(4-hydroxy-iminomethylpyridinium bromide) (C(2)-oxime), NN'-trimethylenebis-(4-hydroxy-iminomethylpyridinium bromide) (C(3)-oxime), NN'-tetramethylene-(4-hydroxy-iminomethylpyridinium bromide) (C(4)-oxime) and NN'-pentamethylenebis-(4-hydroxyiminomethylpyr...

As part of ongoing efforts to design improved nerve agent antidotes, two X-ray crystal structures of Torpedo californica acetylcholinesterase (TcAChE) bound to the bis-pyridinium oxime, Ortho-7, or its experimental bis-imidazolium analogue, 2BIM-7, were determined. Bis-oximes contain two oxime groups connected by a hydrophobic linker. One oxime group of Ortho-7 binds at the entrance to the acti...