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含甲氧基醚键的双吡啶肟对沙林抑制的电鳗乙酰胆碱酯酶的体外重新激活作用。

In vitro reactivation of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing methoxy ether linkages.

作者信息

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

机构信息

Process Technology Development Division, Defence Research and Development Establishment, Jhansi Road, Gwalior 474002, India.

出版信息

Toxicol In Vitro. 2008 Mar;22(2):525-30. doi: 10.1016/j.tiv.2007.10.006. Epub 2007 Oct 25.

Abstract

Bis-pyridinium oximes connected by methoxy alkane ether linker were synthesized and their in vitro reactivation efficacy was evaluated for sarin inhibited AChE. Reactivation efficacy of synthesized compounds was compared with 2-PAM and obidoxime. Among the synthesized compounds, 1,2-dimethoxy ethylene bis-[3,3'-(hydroxyiminomethyl) pyridinium] dichloride (3P-2) and 1,3-dimethoxy propylene bis-[3,3'-(hydroxyiminomethyl) pyridinium] dichloride (3P-3) were found to be most potent reactivators for AChE inhibited by nerve agent sarin. 3P-2 and 3P-3, respectively exhibited 80% and 69% regeneration of inhibited AChE, whereas 2-PAM (well known antidote for nerve agent poisoning) showed 42% regeneration.

摘要

合成了通过甲氧基烷醚连接基连接的双吡啶肟,并评估了它们对沙林抑制的乙酰胆碱酯酶(AChE)的体外重新激活效果。将合成化合物的重新激活效果与2-吡啶醛肟甲基碘(2-PAM)和双复磷进行了比较。在合成化合物中,发现1,2-二甲氧基乙烯双-[3,3'-(羟基亚氨基甲基)吡啶鎓]二氯化物(3P-2)和1,3-二甲氧基丙烯双-[3,3'-(羟基亚氨基甲基)吡啶鎓]二氯化物(3P-3)是对神经毒剂沙林抑制的AChE最有效的重新激活剂。3P-2和3P-3分别使受抑制的AChE有80%和69%的再生,而2-PAM(众所周知的神经毒剂中毒解毒剂)显示有42%的再生。

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