Acharya Jyotiranjan, Gupta Arvind Kumar, Mazumder Avik, Dubey Devendra Kumar
Process Technology Development Division, Defence Research & Development Establishment, Jhansi Road, Gwalior, Madhya Pradesh 474002, India.
Eur J Med Chem. 2009 Mar;44(3):1326-30. doi: 10.1016/j.ejmech.2008.02.020. Epub 2008 Mar 5.
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.
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%。