朱友成, 方苏南. 强效镇痛剂研究 Ⅲ.3,5-桥丙烷基哌啶类衍生物的合成J. 药学学报, 1982, 17(3): 194-199.
引用本文: 朱友成, 方苏南. 强效镇痛剂研究 Ⅲ.3,5-桥丙烷基哌啶类衍生物的合成J. 药学学报, 1982, 17(3): 194-199.
ZHU You-cheng, FANG Su-nan. STUDIES ON POTENT ANALGESICS Ⅲ. SYNTHESIS OF 3,5-PROPANOPIPERIDINE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1982, 17(3): 194-199.
Citation: ZHU You-cheng, FANG Su-nan. STUDIES ON POTENT ANALGESICS Ⅲ. SYNTHESIS OF 3,5-PROPANOPIPERIDINE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1982, 17(3): 194-199.

强效镇痛剂研究 Ⅲ.3,5-桥丙烷基哌啶类衍生物的合成

STUDIES ON POTENT ANALGESICS Ⅲ. SYNTHESIS OF 3,5-PROPANOPIPERIDINE DERIVATIVES

  • 摘要: 本文根据3,5-桥丙烷哌啶类(Ⅰ)及芬太尼类镇痛剂化学结构与药理作用的特点,合成了3-甲基-3,5-桥丙烷基哌啶类衍生物(Ⅳ)及一类新的合并两者结构后的合成镇痛剂N-1-(β-芳乙基)-3-甲基(或氢)-3,5-桥丙烷基哌啶基-N-丙酰芳胺(Ⅲ)。药理初筛表明,所有这些化合物的镇痛强度大多均与吗啡同一水平。

     

    Abstract: According to relationship of chemical structure and analgesic activity between 3,5-propanopiperidine analgesics (Ⅰ) and fentanyl, we prepared 1-(β-phenylethyl)-3-methyl-4-methoxy-4-(m-hydroxyphenyl)-3, 5-propanopiperidine (Ⅳ) and a new series of analgesics e. g. N-1-(β-arylethyl)-3-methyl (or hydrogen)-3,5-propanopiperidyl-N-arylpropanamide(Ⅲ) which combined the structures of the two compounds. Pharmacological results showed that most of these compounds are of the same level of potency as morphine.

     

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