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可逆性胆碱酯酶抑制剂二甲氨基甲酸-[3-(烷氨基)烷氧基-4(5)-叔丁基]苯酯的合成
引用本文:王林,董永明. 可逆性胆碱酯酶抑制剂二甲氨基甲酸-[3-(烷氨基)烷氧基-4(5)-叔丁基]苯酯的合成[J]. 药学学报, 1988, 23(3): 213-217
作者姓名:王林  董永明
作者单位:军事医学科学院毒物药物研究所 北京(王林),军事医学科学院毒物药物研究所 北京(董永明)
摘    要:在催醒安的邻位和对位异构体及其同系物的苯坏上引入烷基后,可以增强抑制胆碱酯酶的活性,我们乃进一步在催醒安及其同系物的苯环不同位置上引入叔丁基,合成了一系列二甲氨基甲酸-[3-(烷氨基)烷氧基-4(5)-叔丁基]苯酯(Ⅰ_(1~13)和Ⅱ_(1~5))(表2),以探索对活性的影响。

关 键 词:胆碱酯酶抑制剂  二甲氨基甲酸-[3-(烷氨基)烷氧基-4-叔丁基]苯酯  二甲氨基甲酸-[3-(烷氨基)烷氧基-5-叔丁基]苯酯
收稿时间:1987-04-15

SYNTHESIS OF 3-(ALKYLAMINO) ALKOXY-4(5)-t-BUTYLPHENYL N, N-DIMETHYLCARBAMATES AS REVERSIBLE CHOLINESTERASE INHIBITORS
L Wang and YM Dong. SYNTHESIS OF 3-(ALKYLAMINO) ALKOXY-4(5)-t-BUTYLPHENYL N, N-DIMETHYLCARBAMATES AS REVERSIBLE CHOLINESTERASE INHIBITORS[J]. Acta pharmaceutica Sinica, 1988, 23(3): 213-217
Authors:L Wang and YM Dong
Abstract:A series of 3-(dialkylamino) alkoxy-4 (5)-t-butylphenyl N, N-dimethylcarbamates(Ⅰ and Ⅱ), which are the nuclear alkylated derivatives of 3-(2-dimethylamino) ethoxyphenyl N, N-dimethylcarbamate (CUI XING AN) was prepared as potential anticholinesterase agents. Preliminary screening tests showed that the introduction of t-butyl group in CUI XING AN and its homologs decreased the toxicity and anticholinesterase activity. Compounds of type Ⅰ have increased protective activity against organophosphorus poisoning.
Keywords:Cholinesterase inhibitor  3-(Alkylamino)alkoxy-4-t-butylphenyl N  N-dimethylcarbamates  3-(Alkylamino)alkoxy-5-t-butylphenyl N  N-dimethylcarbamates
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