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本文报道了一系列N-[-1(2-苯乙基-4-甲氧羰基-4-哌啶基]-N-丙酰苯胺(4-甲氧羰基芬太尼)哌啶环1位取代衍生物的合成及其镇痛活性;讨论了结构与镇痛活性之间的关系。药理试验结果表明,大部分化合物具有典型的吗啡样镇痛活性,是一类作用极强的麻醉性镇痛剂。特别是哌啶环1位β-苯环被取代乙烯基替代的化合物具有相当或接近子母体化合物的镇痛活性。其代表物1321的镇痛活性(ED_(50)=0.005mg/kg ip,小鼠,热板法)略强于4-甲氧羰基芬太尼(ED_(50)=0.0063 mg/kg)。
In this paper, a series of N-1 (2-phenethyl-4-methoxycarbonyl-4-piperidinyl] propionanilide (4-carbomethoxy fentanyl) Substituting derivatives for their analgesic activity and discussing the relationship between structure and analgesic activity.Pharmacological test results show that most of the compounds have a typical morphine-like analgesic activity and are a class of highly-action narcotic Painkillers, in particular piperidine ring substituted at the 1-position β-benzene vinyl substituted compounds have analgesic activity similar or close to the parent compound of its representative compound 1321 analgesic activity (ED 50 = 0.005mg / kg ip, mouse, hot plate method) slightly stronger than 4-methoxycarbonyl fentanyl (ED_ (50) = 0.0063 mg / kg).