Journal of APPLIED BIOMEDICINE
ISSN 1214-0287 (on-line)
ISSN 1214-021X (printed)

Volume 5 (2007), No 1, p 25-30




In vitro reactivation potency of bispyridinium (E)-but-2-ene linked acetylcholinesterase reactivators against tabun-inhibited acetylcholinesterase

Kamil Musilek, Kamil Kuca, Daniel Jun and Martin Dolezal

Address: Department of Toxicology, Faculty of Military Health Sciences, Trebesská 1575, 500 01 Hradec Kralove, Czech Republic
musilek@pmfhk.cz

Received 10th October 2006.
Published online 10th January 2007.

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SUMMARY
Six potential bispyridinium (E)-but-2-ene linked AChE reactivators were tested on tabun-inhibited acetylcholinesterase in vitro. Their reactivation efficacy was compared to currently available AChE reactivators used in the case of organophosphorus intoxications - pralidoxime, HI-6 and obidoxime. According to the results obtained, (E)-1,4'-bis(4-hydroxyiminomethylpyridinium)but-2-ene dibromide (K075) seems to be the most potent reactivator of tabun- inhibited AChE. From the data, the reactivation potency of these compounds depends on structural factors such as the constitution of the linking chain between both pyridinium rings and the position of the oxime moiety at the pyridinium rings.

KEY WORDS
organophosphate; tabun; acetylcholinesterase; reactivation; oxime


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CITED

Bhattacharjee AK, Kuca K, Musilek K, Kuca, K, Gordon RK. An in silico stereo-electronic comparison of conventional pyridinium oximes and K-oximes for organophosphate (OP) poisoning. Med Chem. 8: 230-245, 2012.

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