首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis of a novel series of non-symmetrical bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
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Synthesis of a novel series of non-symmetrical bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.

机译:一系列带有二甲苯连接基的新型非对称双吡啶鎓化合物的合成及其对塔宾和对氧磷抑制的乙酰胆碱酯酶的活化活性评估。

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摘要

Nine potential non-symmetrical xylene-bridged AChE reactivators were synthesized using modifications of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and the insecticide paraoxon together with nine symmetrical xylene-bridged compounds, was tested in vitro. Seven compounds were promising against paraoxon-inhibited AChE. Two compounds were found to be more potent against tabun-inhibited AChE than obidoxime at a concentration applicable in vivo.
机译:使用目前已知的合成途径的修饰方法合成了九种潜在的非对称二甲苯桥联的AChE活化剂。在体外测试了它们被神经毒剂塔文和杀虫剂对氧磷与九种对称的二甲苯桥联化合物抑制的AChE的重新活化能力。七种化合物有望抵抗对氧磷抑制的AChE。在体内适用浓度下,发现两种化合物对烟熏抑制的AChE的作用比奥比多肟更有效。

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