【摘要】 目的:丹皮酚及其类似物通过1,4-二溴丁烷连接,与萘普生反应合成一系列目标产物,研究其抗炎活性。方法:丹皮酚、2-羟基-5-甲氧基-苯乙酮、3-羟基苯乙酮、2-羟基苯乙酮和2,4-二羟基苯乙酮先与1,4-二溴丁烷合成缩合物,再与萘普生合成系列目标化合物。建立了HPLC的含量测定的方法在温度为37℃,p H分别为1.2,5.0和7.4的3种不同缓冲溶液条件下的降解情况,用二甲苯致小鼠耳肿胀模型对其进行抗炎活性筛选。结果:合成了5个目标化合物,经MS和1H-NMR确证其结构。降解试验说明这些化合物在不同p H的缓冲溶液体系中保持稳定。小鼠实验表明,目标化合物具有较强的抗炎作用。结论:目标化合物在胃肠道p H值中稳定,抗炎活性较强,值得进一步研究。更多还原

【Abstract】 Objective: To connect paeonol and its analogs with 1,4-dibromobutane,then to afford a series of target products by reacting with naproxen,and investigate the anti-inflammatory activities of the products.Methods: Paeonol,2-hydroxy-5-methoxyacetophenone,3-hydroxyacetophenone,2-hydroxyacetophenone,and 2,4-dihydroxyacetophenone were condensated with 1,4-dibromobutane,then reacted with naproxen to yield series of target products. An HPLC method was established for determining the content of the target products. Their degradation dynamics was assessed under p H 1. 2,5. 0 and 7. 4 buffer conditions at 37 ℃. The anti-inflammatory activities of the compounds were evaluated in xylene-induced mouse ear swelling model. Results: Five new compounds were synthesized and confirmed by MS and1H-NMR. Degradation kinetic experiments showed that these compounds were stable in buffers of different p Hs. All the compounds showed anti-inflammatory activities. Conclusion: All the compounds are stable and exhibit potent anti-inflammatory activities.更多还原