周德和, 方苏南, 葛邦錀, 李庆祯, 李志毅, 戴淇源, 吴瑞琴, 吴益芝, 黄忠明, 陈新建. 氮杂二环烷类衍生物的合成及其镇痛活性J. 药学学报, 1982, 17(7): 503-509.
引用本文: 周德和, 方苏南, 葛邦錀, 李庆祯, 李志毅, 戴淇源, 吴瑞琴, 吴益芝, 黄忠明, 陈新建. 氮杂二环烷类衍生物的合成及其镇痛活性J. 药学学报, 1982, 17(7): 503-509.
ZHOU De-he, FANG Su-nan, GE Bang-lun, LI Qing-zhen, LI Zhi-yi, DAI Qi-yuan, WU Rui-qin, WU Yi-zhi, HUANG Zhong-ming , CHEN Xin-jian, . SYNTHESIS AND ANALGESIC ACTIVITY OF DERIVATIVES OF AZABICYCLOALKANESJ. Acta Pharmaceutica Sinica, 1982, 17(7): 503-509.
Citation: ZHOU De-he, FANG Su-nan, GE Bang-lun, LI Qing-zhen, LI Zhi-yi, DAI Qi-yuan, WU Rui-qin, WU Yi-zhi, HUANG Zhong-ming , CHEN Xin-jian, . SYNTHESIS AND ANALGESIC ACTIVITY OF DERIVATIVES OF AZABICYCLOALKANESJ. Acta Pharmaceutica Sinica, 1982, 17(7): 503-509.

氮杂二环烷类衍生物的合成及其镇痛活性

SYNTHESIS AND ANALGESIC ACTIVITY OF DERIVATIVES OF AZABICYCLOALKANES

  • 摘要: 本文报道了一系列3-氮杂二环3,3,1-壬旆类Ⅱ和Ⅲ、3-氮杂二环3,2,1-辛烷类Ⅳ和8-氮杂二环3,2,1-辛烷类V相应衍生物的合成及其镇痛活性。经初步药理试验,Ⅱ,Ⅲ与Ⅳ类化合物显示出强的镇痛活性,其中3-(β-苯乙基)-9β-甲氧基-9α-(间-丙酰氧基苯基)-3-氮杂二环3,3,1-壬烷Ⅱα的镇痛强度是吗啡的2000倍。

     

    Abstract: In the present paper, we report the synthesis and analgesic activity of a series of azabicycloalkanes derivatives which are 3-azabicyclo3,3,1nonanes(Ⅱ, Ⅲ), 3-azabicyclo3,2,1.octanes (Ⅳ)and 8-azabicyclo3,2,1octanes (Ⅴ) Preliminary pharmacological results showed that most of the compounds in this series possess strong analgesic activity. The analgesic potency of 3-(β-phenylethyl)-9β-methoxy-9α-(mpropionoxyphenyl)-3-azabicyclo3,3,1 nonane (Ⅱa) corresponds to more than 2000 times that of morphine.

     

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