| 1-(4-烃氧基)苄基四氢异喹啉类化合物及相关化合物的合成与生物活性 |
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| 引用本文： | 何立文,黄文龙,高慧,彭司勋. 1-(4-烃氧基)苄基四氢异喹啉类化合物及相关化合物的合成与生物活性[J]. 药学学报, 1998, 33(10): 741-747 |
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| 作者姓名： | 何立文 黄文龙 高慧 彭司勋 |
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| 作者单位： | 中国药科大学药物化学研究室,南京210009;*中国科学院上海有机所天然产物化学研究室，上海200032 |
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| 摘 要： | 以有心血管活性的异喹啉生物碱为先导物,设计合成了15个3,4-二氢(II1,2)和1,2,3,4-四氢-(4-烃氧基)苄基四氢异喹啉化合物(II3～15)。药理实验表明:大部分化合物有舒张血管条作用,其中化合物II9对低钾诱导的血管收缩有较强的抑制作用,而对高钾诱导的血管收缩无作用,对硝酸乌头碱诱发的大鼠室性心律失常有明显保护作用。
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| 关 键 词： | 异喹啉类 舒张血管条 抗心律失常 |
| 收稿时间： | 1997-10-06 |
SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1-(4-ALKYLOXY)BENZYL-1,2,3,4-TETRAHYDROISOQUINOLINES AND RELATED COMPOUNDS |
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| He Liwen,Huang Wenlong,Gao Hui and Peng Sixun. SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1-(4-ALKYLOXY)BENZYL-1,2,3,4-TETRAHYDROISOQUINOLINES AND RELATED COMPOUNDS[J]. Acta pharmaceutica Sinica, 1998, 33(10): 741-747 |
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| Authors: | He Liwen Huang Wenlong Gao Hui Peng Sixun |
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| Affiliation: | Division of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009. |
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| Abstract: | In an attempt to search for novel cardiovascular drugs which might act on calcium or potassium channels, on the basis of the previous study of our group, 15 1-(4-alkyloxy)benzyl-1,2,3,4-tetrahydroisoquinolines derivatives were designed and synthesized among which 10 were not reported previously in the literature. Preliminary pharmacological studies showed that most of these compounds exhibited relaxation of rat thoria aorta in vitro. Compound III9 exhibited potent inhibiting action on low KCl(20 mmol.L-1)-induced contraction of rat aorta, and significant protective effect on experimental arrhythmia in rats. |
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| Keywords: | Relaxation of rat thoria aortia Antiarrhythmic Isoquinolines |
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