Synthesis and Biological Activity of Some 1,3-Dihydro-2<i>H</i>-3-benzazepin-2-ones with a Piperazine Moiety as Bradycardic Agents
作者:Hong-Yu Liang、Deng-Qing Zhang、Yun Yue、Zhe Shi、Sheng-Yin Zhao
DOI:10.1002/ardp.200900169
日期:2010.1.27
‐ones with a piperazine moiety were designed and synthesized by treating the common intermediate of 1,3‐dihydro‐7,8‐dimethoxy‐3‐[3‐(1‐piperazinyl)propyl]‐2H‐3‐benzazepin‐2‐ones with a variety of N‐aryl‐2‐chloroacetamides and acyl chlorides. Their structures have been characterized by 1H‐NMR, MS, and elemental analysis. The title compounds were evaluated for their bradycardic activity in vitro. Most
通过处理普通中间体1,3-二氢-7,8-二甲氧基-3-[3-(),设计并合成了一系列具有哌嗪部分的1,3-二氢-2H-3-苯并氮杂-2-酮。 1-哌嗪基)丙基]-2H-3-benzazepin-2-ones 与各种 N-芳基-2-氯乙酰胺和酰氯。它们的结构已通过 1H-NMR、MS 和元素分析表征。评价标题化合物的体外心动过缓活性。大多数合成的化合物表现出一定的血管舒张活性和降低心率的活性,并具有心动过缓的效力。