氨甲酰取代的苯氧烷胺衍生物的合成及其活性测试

Synthesis and biological activity of carbamoyl substituted phenoxylalkylamine derivatives

目的设计合成氨甲酰取代的苯氧烷胺类α1-肾上腺素受体(α1-AR)拮抗剂,并研究其对大鼠肛尾肌收缩功能的影响。方法以2,4-二羟基苯甲酸甲酯或2,5-二羟基苯甲酸甲酯为原料,经多步反应合成关键中间体4a、4b,该中间体再与取代苯乙胺经还原胺化反应制得目标化合物,并测试它们对α1-AR的拮抗活性。结果共合成12个新的氨甲酰取代的苯氧烷胺类化合物,其结构经IR、MS、1H-NMR谱确证。结论生物活性测试显示目标化合物均具有一定的α1-AR拮抗作用。

Aim To study the blocking activity of carbamoyl substituted phenoxylalkylamine derivatives as α1-adrenocepter（α1-AR） antagonist.Methods A series of carbamoyl substituted phenoxylalkylamine derivatives were synthesized through the condensation of 4a or 4b with various substituted phenylethanamine and reduction.Results Twelve new compounds were synthesized and their structures were confirmed by MS,^1H-NMR,IR spectra.Their bioactivities had been tested.Conclusion The test result indicated that most the target compounds showed some blocking activity to α1-adrenoceptor.