摘要
目的设计合成具有α、β受体双阻滞作用的系列化合物 ,并进行活性的初步筛选。 方法运用系列化电子等排原理 ,设计合成了系列 1 芳氧基 3 [2 (4 芳酰基哌嗪 )乙氨基 ] 2 丙醇衍生物 ,并经MS、1H NMR、IR确证其结构。结果与结论合成了 15个目标化合物 ,其中 12个为新化合物 ,初步活性测定结果显示 :所合成的化合物均具有α、β受体双阻滞作用。
Aim To design and synthesize a series of compounds possessing α,β -receptor inhibitors.Methods According to the enssitial principal and drug design methods,fifteen compounds of 1-phenoxy-3-(2-piperizinyl)ethylamino-2-propanol were designed and synthesized as α,β -receptor inhibitors.The structures of the compounds were determined by elemental analysis, 1H-NMR and IR.Their activity was tested.Results and Conclusion Fifteen compounds were designed and synthesized,twelve compounds are new compounds.The activity test shows that some compounds have fairly potent α,β -receptor blocking activity.
出处
《中国药物化学杂志》
CAS
CSCD
2003年第3期142-145,共4页
Chinese Journal of Medicinal Chemistry
