奥丙嗪衍生物的合成及其生物活性研究  

Synthesis and biological activities of oxaprozin derivatives

作　　者：项光亚[1] 杨杰[1] 徐喆[1] 石卫华[1] 罗智[1] 

机构地区：[1]华中科技大学同济医学院药学院,湖北武汉430030

出　　处：《中国药物化学杂志》2006年第3期135-139,158,共6页Chinese Journal of Medicinal Chemistry

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。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, Ⅰ a, Ⅰ g and Ⅱ a- 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.

关 键 词：药物化学 化合物制备 化学合成 奥丙嗪 一氧化氮供体 抗炎活性 

分 类 号：R914[医药卫生—药物化学]