| 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 |
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| 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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| 作者姓名： | 李润涛 蔡俊超 蔡孟深 |
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| 作者单位： | 1. 北京医科大学药学院,北京,100083
2. 中国科学院上海药物研究所,上海,200031 |
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| 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。
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| 关 键 词： | 1-烷基-1-苄基-4-(3-氯-2-羟基)丙基哌嗪季铵盐 抗炎活性 镇痛活性 |
| 收稿时间： | 1996-10-27 |
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1-ALKYL-1-BENZYL-4-(3-CHLORO-2-HYDROXY)PROPYL PIPERAZINIUM HALIDES |
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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 HALIDES[J].Acta Pharmaceutica Sinica,1998,33(1):28-33. |
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| Authors: | Li Runtao Cai Junchao Cai Mengshen |
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| Institution: | School of Pharmaceutical Sciences, Beijing Medical University, Beijing 100083. |
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| 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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| Keywords: | Analgesic activity Anti-inflammatory activity 1-Alkyl-1-benzyl-4-(3-chloro-2-hydroxyl) propyl piperazinium halide |
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