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2-芳基咪唑并[1,2-a]吡啶鎓盐的氨基甲酸酯衍生物作为乙酰胆碱酯酶抑制剂和抗有机磷化合物的保护剂。

Carbamate derivatives of 2-arylimidazo[1,2-a]pyridinium salts as acetylcholinesterase inhibitors and protective agents against organophosphorus compounds.

作者信息

Sundberg R J, Dalvie D, Cordero J, Musallam H A

机构信息

Department of Chemistry, University of Virginia, Charlottesville 22901.

出版信息

Chem Res Toxicol. 1993 Jul-Aug;6(4):506-10. doi: 10.1021/tx00034a018.

Abstract

A series of 2-arylimidazo[1,2-a]pyridinium salts with (N,N-dimethylcarbamoyl)oxy or (N-methylcarbamoyl)oxy groups at the 3'- or 4'-position on the phenyl substituent and various substituents on the imidazo[1,2-a]pyridine ring have been synthesized. The compounds show in vitro inhibitory activity against electric eel acetylcholinesterase (AChE), type III, and several of the compounds show protective effects toward the organophosphorus AChE inhibitor soman in mice. The possible structural relationship of these compounds to physostigmine and pyridostigmine is considered.

摘要

已经合成了一系列在苯基取代基的3'-或4'-位带有(N,N-二甲基氨基甲酰基)氧基或(N-甲基氨基甲酰基)氧基且咪唑并[1,2-a]吡啶环上带有各种取代基的2-芳基咪唑并[1,2-a]吡啶鎓盐。这些化合物对电鳗乙酰胆碱酯酶(AChE)III型显示出体外抑制活性,并且其中几种化合物对小鼠体内的有机磷AChE抑制剂梭曼具有保护作用。考虑了这些化合物与毒扁豆碱和吡啶斯的明可能的结构关系。

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