药学学报, 1981, 16(3): 199-210
引用本文:
朱应麒;葛邦錀;方苏南;朱友成;戴淇源;谈宗英;黄忠明;陈新建. 强效镇痛剂研究——Ⅰ.芬太尼类衍生物的合成及其镇痛作用[J]. 药学学报, 1981, 16(3): 199-210.
Zhu Yingqi; Ge Banglun; Fang Sunan; Zhu Youcheng; Dai Qiyuan; Tan Zongying; Huang Zhongming and Ghen Xinjian . STUDIES ON POTENT ANALGESICS Ⅰ.Synthesis and Analgesic Activity of Derivatives of Fentanyl[J]. Acta Pharmaceutica Sinica, 1981, 16(3): 199-210.

强效镇痛剂研究——Ⅰ.芬太尼类衍生物的合成及其镇痛作用
朱应麒;葛邦錀;方苏南;朱友成;戴淇源;谈宗英;黄忠明;陈新建
中国科学院上海药物研究所
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。
关键词:   
STUDIES ON POTENT ANALGESICS Ⅰ.Synthesis and Analgesic Activity of Derivatives of Fentanyl
Zhu Yingqi; Ge Banglun; Fang Sunan; Zhu Youcheng; Dai Qiyuan; Tan Zongying; Huang Zhongming and Ghen Xinjian
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.
Key words:   
收稿日期:
相关功能
PDF(502KB) Free
打印本文
0
作者相关文章