Chin. J. Org. Chem. ›› 2012, Vol. 32 ›› Issue (09): 1719-1724.DOI: 10.6023/cjoc1203131 Previous Articles     Next Articles



吴妍a, 马龙旭a, 牛天巍a, 孟凡领a, 崔勋b, 朴虎日a   

  1. a 延边大学药学院 长白山生物资源与功能分子教育部重点实验室 延吉 133002;
    b 延边大学基础医学院 延吉 133002
  • 收稿日期:2012-03-13 修回日期:2012-05-11 发布日期:2012-04-09
  • 通讯作者: 崔勋, 朴虎日
  • 基金资助:


Synthesis and Positive Inotropic Evaluation of 2-(4-Substituted benzyl-1,4-diazepan-1-yl)-N-(5-bromoquinoxalin-6-yl)acetamides

Wu Yana, Ma Longxua, Niu Tianweia, Meng Fanlinga, Cui Xunb, Piao Huria   

  1. a Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002;
    b College of Medicine, Yanbian University, Yanji 133002
  • Received:2012-03-13 Revised:2012-05-11 Published:2012-04-09
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.81160381)

A series of 2-(4-substituted benzyl-1,4-diazepan-1-yl)-N-(5-bromoquinoxalin-6-yl)acetamides were synthesized and evaluated for their positive inotropic activity by measuring left atrium stroke volume on isolated rabbit-heart preparations. Some of these derivatives exhibited better activity in vitro compared with the existing drug, milrinone, among which N-(5-bromoquinoxalin-6-yl)-2-[4-(4-chlorobenzyl)-1,4-diazepan-1-yl]acetamide (3f) proved to be the most potent, increasing stroke volume by with (6.18±0.06)% [milrinone, (2.46±0.07)%] at a concentration of 3×105mol·L-1. The compounds synthesized were characterized by IR,1H NMR, MS techniques and elemental analysis.

Key words: quinoxaline, 1,4-diazepane, positive inotropic activity, stroke volume