Musilek Kamil, Holas Ondrej, Kuca Kamil, Jun Daniel, Dohnal Vlastimil, Opletalova Veronika, Dolezal Martin
Department of Toxicology, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic.
J Enzyme Inhib Med Chem. 2008 Feb;23(1):70-6. doi: 10.1080/14756360701383981.
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.
通过对现有合成途径进行改进，合成了六种带有（E）-丁-2-烯连接基的乙酰胆碱酯酶单肟-单氨基甲酰重活化剂。在体外测试了它们对被神经毒剂塔崩和杀虫剂对氧磷抑制的乙酰胆碱酯酶的重活化能力。比较了解磷定、HI-6、双复磷、K048、K075和新制备的重活化剂的重活化效果。根据所得结果，一种重活化剂对塔崩抑制的乙酰胆碱酯酶似乎有前景，两种重活化剂对被对氧磷抑制的乙酰胆碱酯酶有前景。对于在4位至少有一个肟基的双季铵盐物质，获得了最佳结果。
