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Chinese Journal of Organic Chemistry >

2012 , Vol. 32 >Issue 9: 1719 - 1724

DOI: https://doi.org/10.6023/cjoc1203131

Articles

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

  • Wu Yan ,
  • Ma Longxu ,
  • Niu Tianwei ,
  • Meng Fanling ,
  • Cui Xun ,
  • Piao Huri
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  • 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 date: 2012-03-13

  Revised date: 2012-05-11

  Online published: 2012-04-09

Supported by

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

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Abstract

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

Cite this article

Wu Yan , Ma Longxu , Niu Tianwei , Meng Fanling , Cui Xun , Piao Huri . Synthesis and Positive Inotropic Evaluation of 2-(4-Substituted benzyl-1,4-diazepan-1-yl)-N-(5-bromoquinoxalin-6-yl)acetamides[J]. Chinese Journal of Organic Chemistry, 2012 , 32(9) : 1719 -1724 . DOI: 10.6023/cjoc1203131

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