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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。
OBJECTIVE: Paeonol and its analogs are linked by 1, 4-dibromobutane and reacted with naproxen to synthesize a series of target products to study their anti-inflammatory activity. Methods: Paeonol, 2-hydroxy-5-methoxy-acetophenone, 3-hydroxyacetophenone, 2-hydroxyacetophenone and 2,4-dihydroxyacetophenone were mixed with 1,4-bis Bromobutane synthesis condensate, and Naproxen synthesis series of target compounds. A HPLC method was developed for the determination of the degradation of mouse ear swelling model under the conditions of 37 ℃ and pH 1.2, 5.0 and 7.4 respectively. The anti-inflammatory activity filter. Results: Five target compounds were synthesized and confirmed by MS and 1H-NMR. Degradation tests showed that these compounds remained stable in buffer systems with different p H. Mouse experiments show that the target compound has a strong anti-inflammatory effect. Conclusion: The target compounds are stable in the p - value of the gastrointestinal tract and have strong anti - inflammatory activity, which deserves further study.