夏霖, 倪沛洲, 吉民. “慢心率”(mexiletine)类似物的合成J. 药学学报, 1984, 19(9): 656-659.
引用本文: 夏霖, 倪沛洲, 吉民. “慢心率”(mexiletine)类似物的合成J. 药学学报, 1984, 19(9): 656-659.
XIA Lin, NI Pei-Zhou , JI Min, . SYNTHESIS OF MEXILETINE ANALOGUESJ. Acta Pharmaceutica Sinica, 1984, 19(9): 656-659.
Citation: XIA Lin, NI Pei-Zhou , JI Min, . SYNTHESIS OF MEXILETINE ANALOGUESJ. Acta Pharmaceutica Sinica, 1984, 19(9): 656-659.

“慢心率”(mexiletine)类似物的合成

SYNTHESIS OF MEXILETINE ANALOGUES

  • 摘要: 本文以2,6-二甲基苯氧乙叉(Ⅱ)为母体,设计合成了苯氧烷胺类(Ⅲ~V),苯氧羟基烷胺类(Ⅵ),N-酰化苯氧烷胺类(Ⅶ),苯甲酸苯氧烷酯类(Ⅷ),苯氧烷胺盐类(Ⅸ)等不同类型的2,6-二甲基苯氧乙叉衍生物。药理试验表明,部分化合物对蟾蜍离体心脏的心跳频率有明显的减慢作用,其中化合物Ⅲa~c和Ⅵa~b,减慢心律作用比“慢心律”(mexiletine)强,部分化合物具有抗惊厥活性。

     

    Abstract: Five types of derivatives related to 1-(2,6-dimethylphenoxy)amino-propane have been synthesized. They are phenoxy-aminopropane (Ⅲ,Ⅴ), phenoxy-hydroxy-aminopropane (Ⅵ), N-acyl-phenoxy-aminoisopropane (Ⅶ), phenoxy-isopropyl ester of benzoic acid (Ⅷ) and phenoxy-isopropyl-ammonium salts (Ⅸ).In preliminary pharmacological assay, some of these compounds exhibited obvious effect of decreasing heart rate on the isolated toad heart. Ⅲ a~c were shown to be more active than mexiletine.In addition, some of the compounds Ⅲa~b, Ⅳa~b, and VIb were found to possess anticonvulsant activity.

     

/

返回文章
返回