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有机磷化合物能抑制乙酰胆碱酯酶(AChE)的活性,吡啶醛肟类季铵盐能与中毒酶的膦酰基发生取代反应使酶恢复活性。本文分别以氧代丙烷和丙烷为桥链,合成了两个系列的不对称3,3′-双吡啶单肟季铵盐,共23个化合物,测定了它们对被二异丙基氟膦酸酯(DFP)抑制AChE的重活化作用,醛肟基的酸离解常数(pK_a)和防护指数(PI),并与氯磷定(2-PAM)和双解磷(TMB-4)进行对比。文中化合物均按如下路线合成:由3-吡啶醛肟与1,3-二氯丙酮或1,3-二溴丙烷制得1-氯-1′-[(3-肟甲基)吡啶鎓]-2-氧
Organophosphorus compounds inhibit acetylcholinesterase (AChE) activity. Pyridine aldoxime quaternary ammonium salts can react with the phosphoryl group of the poisoning enzyme to reactivate the enzyme. In this paper, two series of asymmetric 3,3’-bipyridine monooxime quaternary ammonium salts were synthesized by using propane and propane as bridge respectively. A total of 23 compounds were tested for their ability to react with diisopropylfluorophosphonic acid Ester (DFP) inhibited the reactivation of AChE, the acid dissociation constant (pK_a) and the protective index (PI) of aldoxime, and compared with 2-PAM and TMB-4. The compounds are synthesized as follows: 1-Chloro-1 ’- [(3-oximethyl) pyridinium] is prepared from 3-pyridine aldoxime and 1,3-dichloroacetone or 1,3-dibromopropane -2-oxo