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带有二甲苯连接基的双吡啶肟对沙林抑制的电鳗乙酰胆碱酯酶的体外再生作用

In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker.

作者信息

Acharya Jyotiranjan, Gupta Arvind Kumar, Mazumder Avik, Dubey Devendra Kumar

机构信息

Process Technology Development Division, Defence Research & Development Establishment, Jhansi Road, Gwalior, Madhya Pradesh 474002, India.

出版信息

Eur J Med Chem. 2009 Mar;44(3):1326-30. doi: 10.1016/j.ejmech.2008.02.020. Epub 2008 Mar 5.

Abstract

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.

摘要

合成了一系列通过二甲苯连接基相连的双吡啶肟,并评估了它们对被神经毒剂沙林抑制的乙酰胆碱酯酶(AChE)的体外重活化潜力。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)是对被沙林抑制的AChE最有效的重活化剂。在10分钟内,浓度为10(-4) M时,肟3b使受抑制的AChE再生34%,相比之下,2-PAM和双复磷分别使AChE再生20%和15%。

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