Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase |
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| Authors: | Kamil Musilek Ondrej Holas Kamil Kuca Daniel Jun Vlastimil Dohnal Veronika Opletalova |
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| Affiliation: | 1. Department of Toxicology, Faculty of Military Health Sciences, Trebesska 1575, 500 01, Hradec Kralove, Czech Republic;2. Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05, Hradec Kralove, Czech Republic;3. Department of Food Technology, Mendel University of Agriculture and Forestry Brno, Zemedelska 1, 613 00, Brno, Czech Republic |
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| Abstract: | Six AChE monooxime-monocarbamoyl reactivators with an (E)-but-2-ene linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and insecticide paraoxon was tested in vitro. The reactivation efficacies of pralidoxime, HI-6, obidoxime, K048, K075 and the newly prepared reactivators were compared. According to the results obtained, one reactivator seems to be promising against tabun-inhibited AChE and two reactivators against paraoxon-inhibited AChE. The best results were obtained for bisquaternary substances with at least one oxime group in position four. |
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| Keywords: | acetylcholinesterase reactivation nerve agent tabun pesticide paraoxon reactivator oxime inhibition |
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