Kuca Kamil, Musilek Kamil, Paar Martin, Jun Daniel, Stodulka Petr, Hrabinova Martina, Marek Jan
Center of Advanced Studies, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic.
Molecules. 2007 Aug 20;12(8):1964-72. doi: 10.3390/12081964.
Preparation of 1-(4-hydroxy-iminomethylpyridinium)-3-pyridiniumpropane dibromide is described. This compound represents a new acetylcholinesterase (AChE) reactivator, which has no substituents on the second pyridinium ring as found in other commonly used AChE reactivators. The reactivation ability of this reactivator was tested on tabun- and cyclosarin-inhibited AChE. According to the results obtained, the new compound (without substitution and with decreased molecule size) showed increased reactivation potency in case of cyclosarin inhibited AChE. A potent oxime for treatment of tabun and cyclosarin-caused intoxications was thus obtained via slight modification of the reactivator structure (compared to trimedoxime and K027).
描述了1-(4-羟基-亚氨基甲基吡啶鎓)-3-吡啶鎓丙烷二溴化物的制备方法。该化合物是一种新型乙酰胆碱酯酶(AChE)复活剂,其第二个吡啶鎓环上没有其他常用AChE复活剂中发现的取代基。在塔崩和环沙林抑制的AChE上测试了该复活剂的复活能力。根据所得结果,新化合物(无取代且分子尺寸减小)在环沙林抑制的AChE情况下显示出更高的复活效力。因此,通过对复活剂结构进行轻微修饰(与三甲肟和K027相比),获得了一种用于治疗塔崩和环沙林中毒的强效肟类药物。