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芳环取代桂皮酰胺类化合物的结构与抗惊活性的关系
STRUCTURE-ANTICONVULSANT ACTIVITY RELATIONSHIPS OF SOME CINNAMAMIDES OF SUBSTITUTED AROMATIC RING
【摘要】 <正> 本组以前的工作说明桂皮酰胺类化合物具有不同程度的抗惊活性,而桂皮酰基苯环上的取代基及酰胺基的改变对其抗惊活性有显著的影响。结果显示苯环上取代基的电性效应对抗惊活性有很大的影响,吸电子基可增强活性;取代基(R)与酰胺部分(R′)间存在着适当的搭配,从而获得抗惊作用较强的化合物。为了进一步确证苯环上取代基电性效应对抗惊活
【Abstract】 Twenty-six compounds of halogen, nitro, alkoxy, amino, and acetamino substituted cinnamamides have been synthesized. The coupling constants of the NMR spectra of the protons on the double bond of these compounds demonstrate that their configurations are all trans. The anticonvulsant activity (MES) of 3-chloro and 2,4-dichloro substituted cinnamamides were found to be more potent than other members of the series studied. The anticonvulsant activities of electron donating amino substituted cinnamoyl piperidines are cgmparable with those of the chloro compounds.
- 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1986年07期
- 【被引频次】10
- 【下载频次】40