2008
DOI: 10.1016/j.cbi.2008.04.011
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Oximes: Reactivators of phosphorylated acetylcholinesterase and antidotes in therapy against tabun poisoning

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Cited by 39 publications
(32 citation statements)
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“…Like other previously tested oximes, K203 showed no signifi cant reactivation of tabun-inhibited BChE (14,16). Even after 20 h, the reactivation maximum was only 30 %.…”
Section: In Vitro K203 Interactions With Cholinesterasesmentioning
confidence: 52%
See 1 more Smart Citation
“…Like other previously tested oximes, K203 showed no signifi cant reactivation of tabun-inhibited BChE (14,16). Even after 20 h, the reactivation maximum was only 30 %.…”
Section: In Vitro K203 Interactions With Cholinesterasesmentioning
confidence: 52%
“…Recently we obtained promising results on in vitro reactivation of human AChE inhibited by tabun and antidotal treatment of tabun-poisoned mice with bispyridinium oximes (13)(14)(15)(16)(17)(18). In this paper we tested the reactivation and antidotal potency of bispyridinium oxime K203, which is an analogue of the most effi cient oxime from our previous studies, K048 (Figure 1) (13,14).…”
mentioning
confidence: 99%
“…24,31 Oxime functional group is essential for reactivation process. For POX-inhibited AChE, at least one oxime group in position four (30) seemed to be beneficial, when compared to related compounds with the oxime in position two (17,28) or three (18,29), especially for 10 µM. Compounds with oxime group in position 3 were much less effective (26 compared to 25 and 27) that was formerly explained by increased pKa of 3-positioned oxime.…”
Section: Resultsmentioning
confidence: 99%
“…16 Reactivators are monoquaternary or bisquaternary pyridinium salts, which bear an oxime (hydroxy- iminomethyl) group in the molecule. 17,18 Dissociated oximate anion is able to attack to the covalent bond in the AChE-OPC complex and restores the enzyme function. 19 The pralidoxime (1, 2-hydroxyiminomethyl-1-methylpyridinium chloride), HI-6 (2, 1-(2-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-2-oxapropane dichloride) obidoxime (3, 1,3-bis(4-hydroxyiminomethylpyridinium)-2-oxapropane dichloride) are commercially available oxime reactivators 20 ( Figure 2).…”
Section: Introductionmentioning
confidence: 99%
“…Pretreatment with oximes is possible, because oximes in addition to their reactivation potency also act as protectors of AChE against phosphorylation, by reversible inhibition of the enzyme 11,12 . Based on our promising results from previous studies with K-oximes [13][14][15][16][17] , we decided to test the two most potent AChE reactivators, oximes K074 and K048, in combination with atropine in the pretreatment and therapy of tabun-poisoned mice. This study was conducted to determine whether oxime In vivo experimental approach to treatment against tabun poisoning and atropine in pretreatment would improve the efficacy of a standard therapy regimen.…”
Section: Introductionmentioning
confidence: 99%