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本文报道了以中草药有效成分为先导物,设计合成了111个异喹啉衍生物包括双苄基异喹啉、苄基异喹啉、原小檗碱等类型化合物,对所合成衍生物进行α-受体,腺苷A1,A2,DHP钙通道放射受体分析以及其它的心血管活性研究,发现化合物VI_(19)具有α_1-受体拮抗作用新的钾通道阻滞剂,V_9和 V_(21)可降低多种动物模型的血压,而无反射性加速心律的副作用,VI_(13)具有抗心律失常和抗室颤作用,该化合物有可能进入临床试验。本文总结了部分化合物的构效关系为进一步研究新化合物提供理论基础。
In this paper, 111 isoquinoline derivatives including bisbenzyl isoquinoline, benzyl isoquinoline and protoberberine were designed and synthesized based on the active ingredients of Chinese herbal medicine. The synthesized derivatives of α - Receptor, Adenosine A1, A2, DHP Calcium Channel Radioreceptor Assay and Other Cardiovascular Activity Studies. It was found that compound VI_ (19) possesses α_1-receptor antagonism. New potassium channel blockers, V_9 and V_ 21) can reduce blood pressure in a variety of animal models, without reflex to accelerate the side effects of heart rhythm, VI_ (13) has anti-arrhythmia and anti-ventricular fibrillation, the compound is likely to enter clinical trials. This article summarizes the structure-activity relationship of some compounds to provide a theoretical basis for further research on new compounds.