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.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第3期135-139,158,共6页
Chinese Journal of Medicinal Chemistry
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
medicinal chemistry
compound preparation
chemical synthesis
oxaprozin
nitric oxide donor
anti-inflammatory activity
