【摘要】 本文报道了芬太尼类衍生物的化学结构与镇痛活性之间的关系。分别改变了芬太尼中的哌啶环1位氮原子的取代基,N-酰芳胺基及哌啶环等部分结构。药理试验结果表明,大部分化合物均具有吗啡样镇痛活性,其镇痛强度分别为吗啡的2～150倍左右。更多还原

【Abstract】 In the present paper, we report the preparation of a series of Fentanyl derivatives which are N-[1-(β-arylalkyl)-4-piperidyl]-N-propionyl aniline, N-[1-(β-phenylet-hyl)-4-piperidyl]-N-amidoaniline, N-[1(-β-phenylethyl)-4-piperidyl]-E-propionylary-lamine, N-[1-(β-arylethyl)-4-tropyl]-N-propionyl aniline and N-1-(β-arylethyl)-4-pyrrolidinyl]-N-propionyl aniline. A total of 22 compounds were synthesized.Pharmacological results showed that most of the compounds in these series possessed morphine-like effects in laboratory animals with potencies levels 2～150 times those of morphine.更多还原