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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。9. N-杂环丙烯醛肟甲基碘化物。

Structure-activity relationships in reactivators of organophosphorus-inhibited acetylcholinesterase. 9. N-Heterocyclic acraldoximes methiodides.

作者信息

Franchetti P, Grifantini M, Martelli S

出版信息

J Med Chem. 1975 Aug;18(8):839-42. doi: 10.1021/jm00242a017.

DOI:10.1021/jm00242a017
PMID:1159702
Abstract

N-Heterocyclic acraldoximes methiodides, where the heterocyclic residues are 2-, 3-, and 4-pyridyl, 2-(1-methyl)imidazolyl or 4-pyrimidyl, were prepared and tested for their reactivating potency on acetylcholinesterase inhibited from diisopropylphosphorofluoridate (DFP). The in vitro testing revealed that the new compounds are good reactivators of the phosphorylated electric eel cholinesterase. The structure-activity relationships are briefly discussed.

摘要

N-杂环丙烯醛肟甲基碘化物,其杂环残基为2-、3-和4-吡啶基、2-(1-甲基)咪唑基或4-嘧啶基,已被制备并测试了它们对由二异丙基氟磷酸酯(DFP)抑制的乙酰胆碱酯酶的复活效力。体外测试表明,这些新化合物是磷酸化电鳗胆碱酯酶的良好复活剂。简要讨论了构效关系。

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J Med Chem. 1975 Aug;18(8):839-42. doi: 10.1021/jm00242a017.
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