异喹啉类心血管药物研究进展

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异喹啉类心血管药物研究进展

彭司勋, 华维一, 黄文龙, 黄枕亚, 蔡惠民

中国药科大学药物化学研究室, 南京 210009

收稿日期:1992-06-16 修回日期:1992-09-25 出版日期:1993-06-15 发布日期:1993-06-15

Development of Cardiovascular Drugs Based on Isoquinoline Compounds from Chinese Medicinal Materials

Si-Xun Peng, Wei-Yi Hua, Wen-Long Huang, Zhen-Ya Huang, Hui-Ming Cai

Division of Medicinal Chemistry China Pharmaceutical University, Nanjing 210009

Received:1992-06-16 Revised:1992-09-25 Online:1993-06-15 Published:1993-06-15

摘要/Abstract

摘要： 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VI19具有α1-受体拮抗作用新的钾通道阻滞剂, V9和V21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, VI13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。

关键词: 异喹啉化合物, 心血管药物

Abstract: By using active principles of Chinese medicinal materials as lead compounds soquinoline derivatives have been designed and synthesized. Their chemical structures include bisbenzylisoquinoline, benzyl-isoquinoline and protoberberine. Their cardiovascular effects were studied involving α-adrenoceptor, adenosine A1, A2 and DPH-calcium channel radioreceptor assays.In addition, calmodulin inhibiting, calcium antagonistic potassium channel blocking and antiplatelet aggregation activities were also performed.It was found that compound VI19 was a new potassium channe blocker with α-adrenoceptor antagonism, compound V9, and V21 lowered blood pressure on various animal models with negative chronotropic action, compound VI13 possessed antiarrhythmic and antifi- brillation action, and it may be a candidate tot clinic evaluation.The structure-activity relationships deduced may provide a theoretical basis for further development of new agents.

Key words: Isoquinoline compounds, Cardiovascular drugs

Supporting:

彭司勋, 华维一, 黄文龙, 黄枕亚, 蔡惠民. 异喹啉类心血管药物研究进展[J]. .

Si-Xun Peng, Wei-Yi Hua, Wen-Long Huang, Zhen-Ya Huang, Hui-Ming Cai. Development of Cardiovascular Drugs Based on Isoquinoline Compounds from Chinese Medicinal Materials[J]. .