Kinetic assessment of N-methyl-2-methoxypyridinium species as phosphonate anion methylating agents.
Kinetic assessment of N-methyl-2-methoxypyridinium species as phosphonate anion methylating agents.
复制标题
N-甲基-2-甲氧基吡啶鎓类作为膦酸根阴离子甲基化剂的动力学评估。
DOI：
10.1021/ol400054m
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发表时间：
2013
期刊：
影响因子：
5.2
通讯作者：
Quinn,DanielM
中科院分区：
文献类型：
--
作者：
Topczewski,JosephJ;Quinn,DanielM
有机磷神经毒剂和杀虫剂是乙酰胆碱酯酶 (AChE) 的有效抑制剂。尽管肟亲核试剂可以重新激活乙酰胆碱酯酶-磷加合物，但该加合物会发生称为老化的反应。没有描述过能够重新激活老化的乙酰胆碱酯酶加合物的化合物。提出了在模型系统中逆转衰老的 2-甲氧基吡啶鎓家族。该系统的动力学研究（包括 SAR 分析）表明，该反应基于环取代基是高度可调的。
Organophosphate nerve agents and pesticides are potent inhibitors of acetylcholinesterase (AChE). Although oxime nucleophiles can reactivate the AChE-phosphyl adduct, the adduct undergoes a reaction called aging. No compounds have been described that reactivate the aged-AChE adduct. A family of 2-methoxypyridinium species which reverse aging in a model system is presented. A kinetic study of this system, which includes an SAR analysis, demonstrates that the reaction is highly tunable based on the ring substituents.