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

doi:10.6023/cjoc1203131

Chin. J. Org. Chem. ›› 2012, Vol. 32 ›› Issue (9): 1719-1724.DOI: 10.6023/cjoc1203131 Previous Articles Next Articles

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2-(4-取代苄基-1,4-高哌嗪-1-基)-N-(5-溴喹喔啉-6-基)乙酰胺衍生物的合成及正性肌力活性研究

吴妍^a, 马龙旭^a, 牛天巍^a, 孟凡领^a, 崔勋^b, 朴虎日^a

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 E-mail:piaohuri@yahoo.com.cn
基金资助:
国家自然科学基金(No.81160381)资助项目

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

Wu Yan^a, Ma Longxu^a, Niu Tianwei^a, Meng Fanling^a, Cui Xun^b, Piao Huri^a

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

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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]. Chin. J. Org. Chem., 2012, 32(9): 1719-1724.

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2-(4-取代苄基-1,4-高哌嗪-1-基)-N-(5-溴喹喔啉-6-基)乙酰胺衍生物的合成及正性肌力活性研究

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

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