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有机化学 ›› 2006, Vol. 26 ›› Issue (11): 1576-1583. 上一篇    下一篇

研究论文

哒嗪酮类α1-肾上腺素受体拮抗剂的合成和生物活性研究

习保民a，江振洲b，王涛b，倪沛州*,c   

  1. (a中国药科大学物理化学教研室 南京 210038)
    (b中国药科大学新药筛选中心 南京 210038)
    (c中国药科大学有机化学教研室 南京 210038)
  • 收稿日期:2006-02-06 修回日期:1900-01-01 发布日期:2006-10-27
  • 通讯作者: 倪沛州

Studies on Synthesis and Biological Activity of Pyridazinone Derivatives as α1-Adrenoceptor Antagonist

XI Bao-Mina,JIANG Zhen-Zhoub,WANG Taob,NI Pei-Zhou*,c   

  1. (a Department of Physical Chemistry, China Pharmaceutical University, Nanjing 210038)
    (b National Drug Screening Center , China Pharmaceutical University, Nan-jing 210038)
    (c Department of Organic Chemistry, China Pharmaceutical University, Nanjing 210038)
  • Received:2006-02-06 Revised:1900-01-01 Published:2006-10-27
  • Contact: NI Pei-Zhou

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将苯(氧)乙胺和苯氧烷胺类α1-肾上腺素受体拮抗剂中的苯(氧)乙胺、苯氧烷胺片段引入哒嗪酮类化合物中, 设计、合成了30个新的含哒嗪酮环的α1-肾上腺素受体拮抗剂. 所有新化合物的结构均经1H NMR, IR, HRMS确证. 生物活性测试表明28个目标物对α1-肾上腺素受体有较好的拮抗作用(pA2＞6.00), 化合物6o, 6p, 6q, 6v, 6x, 6y, 10c, 10d的pA2值＞7.00.

关键词: 哒嗪酮, 合成, α1-肾上腺素受体拮抗剂, 生物活性

Phenylethylamine and phenoxylalkylamine fragments were introduced into pyridazinone derivatives (as α1-adrenoceptor antagonist) for the first time. 30 new compounds of pyridazinone were designed and synthesized. The structures of the new compounds were identified by 1H NMR, IR and HRMS spectra. Target compounds have been assayed with function analysis in anococcyeus muscle. The results indicate that 28 target compounds have good blocking activity to α1-adrenoceptor (pA2＞6.00), The pA2 of compounds 6o, 6p, 6q, 6v, 6x, 6y, 10c and 10d were beyond 7.00.

Key words: synthesis, biological activity, α1-adrenoceptor antagonist, pyridazinone