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有机磷抑制的乙酰胆碱酯酶重活化剂的构效关系。10. 羟基亚胺甲基芳基乙烯基吡啶甲碘化物。

Structure-activity relationships in reactivators of organophosphorus-inhibited acetylcholinesterase. 10. Hydroxyiminomethylarylethenylpyridine methiodides.

作者信息

Arena F, Manna F, Pizza C, Stein M L, Grifantini M

出版信息

J Med Chem. 1975 Nov;18(11):1147-50. doi: 10.1021/jm00245a022.

Abstract

The synthesis of styrylpyridine methiodides where a hydrogen of the pyridyl moiety was replaced by the hydroxyiminomethyl group produced highly effective inhibitors of acetylcholinesterase. As starting materials 4-methylpyridine-2-aldoxime and 2-methylpyridine-4-aldoxime methiodides were prepared which, together with 4-imidazolylethenyl-pyridine-2-aldoxime methiodide, were the only substances for which some activity as reactivators of phosphorylated electric eel cholinesterase in vitro could also be found.

摘要

将吡啶基部分的一个氢被羟基亚氨基甲基取代的苯乙烯基吡啶甲基碘化物合成得到了高效的乙酰胆碱酯酶抑制剂。制备了4-甲基吡啶-2-醛肟和2-甲基吡啶-4-醛肟甲基碘化物作为起始原料,它们与4-咪唑基乙烯基吡啶-2-醛肟甲基碘化物一起,是仅有的在体外对磷酸化电鳗胆碱酯酶具有一些作为重活化剂活性的物质。

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