可逆性胆碱酯酶抑制剂 Ⅱ.二甲氨基甲酸间-(烷氨基)烷硫基苯酯的合成

前文报道了一系列二甲氨基甲酸间-(烷氨基)烷氧基苯酯(I,X=O)的合成,发现催醒安(I,X=O,n=2,R=CH_3)对临床中麻催醒有较好的效果,是一个结构简单、易于合成、具有中枢作用的可逆性胆碱酯酶抑制剂。但催醒安对中枢胆碱酯酶的抑制作用不够强,为此,我们合成了相应的硫代衍生物(Ⅱ,X=S)(表2)以期能增强对中枢胆碱酯酶的抑制作用。

STUDIES ON REVERSTBLE CHOLINESTERASE INHIBITORS.Ⅱ.SYNTHESIS OF m-(ALKYLAMINO) ALKYLTHIOPHENYL N,N-DIMETHYLCARBAMATES

In a previous paper we have described the synthesis and biological evaluation of some m-(alkylamino) alkoxyphenyl N, N-dimethylcarbamates. One of these compounds, CUI XING AN, is now used as an analeptic for Chinese traditional herbal anesthesia. In order to search for further anticholinesterases with higher activity on the CNS, a number of thio-analogues of the above series were synthesized. Several of these compounds were found to have much higher anticholinesterase activity than the corresponding oxygen analogues, among which m-(2-diethylamino)-ethylthiophenyl-N, N-dimethylcarbamate (Ⅱ₂) was shown to be the most active. Compound Ⅱ₂ exhibited a longer duration of action in animal experiments than CUI XING AN.