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奥丙嗪衍生物的合成及其生物活性研究

Synthesis and biological activities of oxaprozin derivatives

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【作者】 项光亚杨杰徐喆石卫华罗智

【Author】 XIANG Guang-ya,YANG Jie,XU Zhe,SHI Wei-hua,LUO Zhi(Pharmacy School of Tongji Medical College,Huazhong University of Science and Technology,Wuhan 430030,China)

【机构】 华中科技大学同济医学院药学院华中科技大学同济医学院药学院 湖北武汉430030湖北武汉430030

【摘要】 目的设计合成一系列NO供体型奥丙嗪,并考察它们的体外NO释放活性与抗炎活性。方法以奥丙嗪为原料,利用其羧基将奥丙嗪与呋咱环结构或硝酸酯结构偶联起来,得到NO供体型奥丙嗪。结果与结论合成11个NO供体型奥丙嗪衍生物,其中化合物Ⅰa、Ⅰg和Ⅱa~Ⅱd6个化合物为新化合物,目标化合物的结构经MS和1H-NMR确认。呋咱环型化合物在体外能有效地释放出NO,大多数化合物仍保持抗炎活性。

【Abstract】 Aim To design and synthesize a serial of NO-releasing oxaprozin derivatives,and to study their NO-releasing ability in vitro and their anti-inflammatory activities.Methods NO-releasing oxaprozin derivatives were synthesized by coupling oxaprozin with furoxan or nitrate ester moieties through the carboxyl group of oxaprozin.Results and conclusion NO-releasing oxaprozin compounds were synthesized.Among these,Ⅰa,Ⅰg and Ⅱa~Ⅱd are new compounds.The target compounds were confirmed by MS and()~1H-NMR.Furoxan-type compounds can release NO effectively in vitro,and most of the target compounds maintain anti-inflammatory activities.

  • 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2006年03期
  • 【分类号】R914
  • 【被引频次】2
  • 【下载频次】127
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