首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker.
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In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker.

机译:沙林的体外再生通过带有二甲苯连接基的双吡啶肟抑制电鳗乙酰胆碱酯酶。

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摘要

A series of bis-pyridinium oximes connected by xylene linker were synthesized and their in-vitro reactivation potential was evaluated against acetylcholinesterase (AChE) inhibited by nerve agent, sarin. Among the synthesized compounds, alpha,alpha'xylene-bis-[3,3'-(hydroxyiminomethyl) pyridinium] dibromide (3b) was found to be most potent reactivator for AChE inhibited by sarin. The oxime 3b exhibits 34% regeneration of inhibited AChE, in comparison to 20 and 15% regeneration by 2-PAM and obidoxime, respectively, at a concentration of 10(-4) M within 10 min.
机译:合成了一系列通过二甲苯连接基连接的双吡啶肟,并评估了它们在体外被神经毒剂沙林抑制的乙酰胆碱酯酶(AChE)的体外再活化潜力。在合成的化合物中,发现α,α'二甲苯-双-[​​3,3'-(羟基亚氨基甲基)吡啶鎓]二溴化物(3b)是沙林抑制的最有效的AChE活化剂。在10分钟内浓度为10(-4)M的情况下,肟3b表现出34%的受抑制的AChE再生,而2-PAM和Obidoxime的再生分别为20%和15%。

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