李润涛, 蔡俊超, 蔡孟深. 1-烷基-1-苄基-4-(3-氯-2-羟基)丙基哌嗪季铵盐的合成及生物活性J. 药学学报, 1998, 33(1): 28-33.
引用本文: 李润涛, 蔡俊超, 蔡孟深. 1-烷基-1-苄基-4-(3-氯-2-羟基)丙基哌嗪季铵盐的合成及生物活性J. 药学学报, 1998, 33(1): 28-33.
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Li Runtao, Cai Junchao , Cai Mengshen, . SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1-ALKYL-1-BENZYL-4-(3-CHLORO-2-HYDROXY)PROPYL PIPERAZINIUM HALIDESJ. Acta Pharmaceutica Sinica, 1998, 33(1): 28-33.
Citation: Li Runtao, Cai Junchao , Cai Mengshen, . SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1-ALKYL-1-BENZYL-4-(3-CHLORO-2-HYDROXY)PROPYL PIPERAZINIUM HALIDESJ. Acta Pharmaceutica Sinica, 1998, 33(1): 28-33.
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1-烷基-1-苄基-4-(3-氯-2-羟基)丙基哌嗪季铵盐的合成及生物活性

SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1-ALKYL-1-BENZYL-4-(3-CHLORO-2-HYDROXY)PROPYL PIPERAZINIUM HALIDES

    摘要
  • 摘要: 设计合成了7个1-烷基-1-苄基-4-(3-氯-2-羟基)丙基哌嗪季铵盐(Ia～g)。生物活性试验结果表明,苄基苯环上连有强吸电子取代基时,可使抗炎和镇痛活性明显增强;季铵盐中的负离子对生物活性有一定的影响。在20mg·kg-1的剂量下,Id和Ie的抗炎活性和Ie的镇痛活性明显。

     

    Abstract: Seven 1-alkyl-1-benzyl-4-(3-chloro-2-hydroxy) propyl piperazinium halide hydrochloride were synthesized. Preliminary biological activity test showed that the presence of electroattracting group in the benzyl distinctly increased the analgesic and antiinflammatory activities of the compounds. For example, the analgesic activity of Ie and the antiinflammatory, activities of Id and Ie were all higher than those of Ia and Ib. The different anion of quaternary ammonium have some effect on the biological activity. However, this effect is not regular.

     

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