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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   

  1. 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

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

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