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.
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 , Ghen Xinjian, . STUDIES ON POTENT ANALGESICS Ⅰ.Synthesis and Analgesic Activity of Derivatives of FentanylJ. Acta Pharmaceutica Sinica, 1981, 16(3): 199-210.
Citation: Zhu Yingqi, Ge Banglun, Fang Sunan, Zhu Youcheng, Dai Qiyuan, Tan Zongying, Huang Zhongming , Ghen Xinjian, . STUDIES ON POTENT ANALGESICS Ⅰ.Synthesis and Analgesic Activity of Derivatives of FentanylJ. 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

STUDIES ON POTENT ANALGESICS Ⅰ.Synthesis and Analgesic Activity of Derivatives of Fentanyl

  • 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。

     

    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.

     

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