Synthesis of Bispyridinium Compounds Bearing Propane Linker and Evaluation of their Reactivation Activity against Tabun- and Paraoxon-Inhibited Acetylcholinesterase

Title: Synthesis of Bispyridinium Compounds Bearing Propane Linker and Evaluation of their Reactivation Activity against Tabun- and Paraoxon-Inhibited Acetylcholinesterase

Volume: 3 Issue: 11

Author(s): Kamil Musilek, Ondrej Holas, Jan Hambalek, Kamil Kuca, Daniel Jun, Vlastimil Dohnal and Martin Dolezal

Affiliation:

Keywords: Acetylcholinesterase, reactivation, tabun, paraoxon, reactivator, oxime

Abstract: Six AChE reactivators with propane linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by nerve agent tabun and insecticide paraoxon was tested in vitro. The reactivation efficacies of pralidoxime, HI-6, obidoxime and six synthesized reactivators were compared. According to the results obtained, three reactivators seem to be promising against paraoxon-inhibited AChE. Better results were obtained for bisquaternary substances at least with one oxime group in position four. None of the tested substances was able to satisfactorily reactivate tabun-inhibited AChE.

Cite this article as:

Musilek Kamil, Holas Ondrej, Hambalek Jan, Kuca Kamil, Jun Daniel, Dohnal Vlastimil and Dolezal Martin, Synthesis of Bispyridinium Compounds Bearing Propane Linker and Evaluation of their Reactivation Activity against Tabun- and Paraoxon-Inhibited Acetylcholinesterase, Letters in Organic Chemistry 2006; 3 (11) . https://dx.doi.org/10.2174/157017806779117012