| 抗心律失常药物的研究──Ⅰ、苯丙二醇胺类化合物的合成及生物活性 |
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| 引用本文： | 王如斌,彭司勋,华维一. 抗心律失常药物的研究──Ⅰ、苯丙二醇胺类化合物的合成及生物活性[J]. 山东大学学报(医学版), 1994, 0(2) |
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| 作者姓名： | 王如斌 彭司勋 华维一 |
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| 作者单位： | 中国药科大学药物化学研究室 |
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| 摘 要： | 设计合成了１２个苯丙二醇胺类化合物，其中１１个未见文献报道，其化学结构经红外光谱、核磁共振、质谱和元素分析证实。经抗氯仿诱发小鼠心律失常试验表明，Ⅰ_１、Ⅰ_２、Ⅰ_３、Ⅰ_７和Ⅰ_８５个化合物具有明显的抗心律失常活性。
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| 关 键 词： | 抗心律失常药，苯丙二醇胺，药物筛选 |
STUDIES ON ANTIARRHYTHMIC AGENTS I.SYNTHESIS OF 1-PHENYL-3-ALKYLAMINO1,2-PROPANEDIOL ANALOGUES AND SCREENING FOR THEIR ANTIARRHYTHMIC ACTIVITY |
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| Wang Rubin, Peng Sixun, Hua Weiyi. STUDIES ON ANTIARRHYTHMIC AGENTS I.SYNTHESIS OF 1-PHENYL-3-ALKYLAMINO1,2-PROPANEDIOL ANALOGUES AND SCREENING FOR THEIR ANTIARRHYTHMIC ACTIVITY[J]. Journal of Shandong University:Health Sciences, 1994, 0(2) |
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| Authors: | Wang Rubin Peng Sixun Hua Weiyi |
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| Abstract: | Twelve PhCH (OH) CH ( OH ) CH2NR1R2 ( R1, R2 =alkyl ,arylalkyl; R1and R2 may form a ring ) were prepared by halogenation of phCH=CHCH2OH, reaction with HNR1R2, acylation, then oxidation and hydrolysis. Thus, treatment of phCH=CHCH2OH with SOCl2gave 57% phCH=CHCH2Cl, which (15.3g) was refluxed with 50ml Me2CHNH2 12h to give 80% phCH=CHCH2NHCHMe2. Acetylation of 2 gave phCH= CHCH2N ( Ac) CHMe2, which ( 7.6g) in EtOH was oxidized with 7.75g KMno4 and 4g MgSO4 to give 45.5% phCH (OH) CH (OH) CH2N (Ac) CHMe2.Hydrolysis of it with 10% aqueous NaOH in EtOH gave 82% phCH (OH) CH (OH) CH2NHCHMe2. Screening test indicated that I1,I2,I3, I7 and I 8 could markedly antagonize CHCl3-induced arrhythmias in rats. |
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| Keywords: | Antiarrhythmics Phenylpropanediolamine Drug screening |
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