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2-或5-取代的六氢-1H.1,4-二氮(?)类化合物(1~3)经单酰化及酰化反应后,合成了16个带有(1-芳乙酰胺基-2-叔氨基)乙烷结构的六氢-1H-1,4-二氮(?)类目标化合物(5~9,11~13,15~17,19~23),经元素分析、IR、MS和1H NMR确证了其组成和结构.对所有目标化合物都进行了豚鼠回肠试验,初步药理试验表明,16个化合物对受试标本显示不同程度的抑制作用,对抑制率较高的两个化合物5和7测试了IC50值.对在豚鼠回肠试验中显示较强激动作用的4个化合物进行了小鼠扭体法镇痛活性试验,测得了其ED50值.
2- or 5-substituted hexahydro-1H. After the mono-acylation and acylation of 1,4-diazepan compounds (1 ~ 3), sixteen hexaazoles with six (1-arylacetamido-2-tertiary amino) Hydrogen-1H-1,4-diazide target compounds (5 ~ 9,11 ~ 13,15 ~ 17,19 ~ 23) were confirmed by elemental analysis, IR, MS and 1H NMR . Guinea pig ileum test was performed on all the target compounds. Preliminary pharmacological tests showed that 16 compounds showed different degrees of inhibition on the tested samples, and IC50 values of two compounds 5 and 7 with higher inhibition rates were tested. Four compounds that showed a strong agonistic effect in guinea pig ileum test were tested for writhing analgesic activity and their ED50 values were measured.