由于粉防己碱裂解产物具有α-受体拮抗活性。结合钙拮抗剂某些结构特征,设计合成了一系列取代的苄基异喹啉衍生物,药理试验表明所合成化合物对α-受体具有不同程度的亲和力。为探索构效关系测定了所合成化合物HPLC保留因子(logK’),以此作为疏水参数结合其它的结构参数与α_1-受体亲和力进行Hansch分析,结果表明活性与取代基的疏水值π,共轭效应R正相关,与摩尔折射度MR负相关。 Tetrandrine lysates have alpha -receptor antagonistic activity. In combination with some structural features of calcium antagonists, a series of substituted benzylisoquinoline derivatives were designed and synthesized. Pharmacological experiments show that the synthesized compounds have different degrees of affinity for α-receptors. In order to explore the structure-activity relationship of compounds synthesized by HPLC retention factor (logK ’), as a hydrophobic parameter combined with other structural parameters and α_1-receptor affinity Hansch analysis, the results show that the activity and substituent hydrophobic π, The yoke effect R is positively correlated and negatively correlated with the molar refraction MR.