【摘要】 目的合成一氧化氮(NO)供体型阿司匹林和水杨酸甲酯,并检测其体外释放NO的能力和抗炎活性。方法通过酯键和醚键将阿司匹林和水杨酸甲酯分别与NO供体结构偶联,利用Griess试剂检测其释放NO的活性,并用二甲苯致小鼠耳肿胀模型初步研究其抗炎活性。结果合成了6种化合物,其中4种在体外具有良好的NO释放能力,6种化合物均保持有抗炎活性。结论所有化合物的结构均经MS1、H-NMR确证,呋咱环型化合物体外能有效释放NO,NO供体结构的引入对其母体化合物的抗炎活性影响甚微。更多还原

【Abstract】 Objective To synthesize nitric oxide(NO)-releasing aspirin and methyl salicylate,and detect their NO-releasing ability in vitro and anti-inflammatory activities.Methods Aspirin and methyl salicylate were coupled with NO-releasing groups through ester and ether bonds.NO-releasing ability was tested by Griess regent.Xylene-induced mice ear edema model was used to study their anti-inflammatory activities.Results Six compounds were synthesized and confirmed by MS,1H-NMR.Four of these compounds had good ability to release NO in vitro.All compounds maintained their anti-inflammatory activities.Conclusion All compounds were confirmed by MS and 1H-NMR.Furoxan-type compounds could release NO effectively,and NO-donor group had little effect on their anti-inflammatory activities.更多还原