Acharya Jyotiranjan, Gupta Arvind Kumar, Mazumder Avik, Dubey Devendra Kumar
Process Technology Development Division, Defence Research and Development Establishment, Jhansi Road, Gwalior 474002, India.
Toxicol In Vitro. 2008 Mar;22(2):525-30. doi: 10.1016/j.tiv.2007.10.006. Epub 2007 Oct 25.
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.
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。