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依据活性结构单元的拼合原理,以2-呋喃甲醛和4-氟苯乙酮为原料出发,经Aldol缩合、脱水、哌嗪取代反应生成4’-(1-哌嗪基)呋喃查尔酮(2)后,再与酰氯和磺酰氯反应,得到了10个未见报道的含哌嗪取代的呋喃查尔酮衍生物,其结构经~1H NMR和~(13)C NMR确证。采用小鼠巨噬细胞Raw 264.7模型初步测试了目标化合物的体外抗炎活性,结果表明,磺酰胺类化合物的抗炎活性要优于酰胺类化合物,特别是化合物4d能有效抑制NO的生成(IC_(50)=3.88μmol/L),与阳性对照药地塞米松活性相当。
According to the principle of the assembly of the active structural units, 2-furfuraldehyde and 4-fluoroacetophenone were used as starting materials to produce 4 ’- (1-piperazinyl) furan chalcone by Aldol condensation, dehydration and piperazine substitution 2), and then reacted with acid chloride and sulfuryl chloride to obtain 10 unreported piperazine substituted furan chalcone derivatives. The structures were confirmed by ~ 1H NMR and ~ (13) C NMR. The anti-inflammatory activity of the target compounds was tested in vivo using Raw 264.7 model of mouse macrophages. The results showed that the anti-inflammatory activity of the sulfonamides was better than that of the amide compounds. In particular, compound 4d could effectively inhibit the production of NO (IC_ (50) = 3.88μmol / L), comparable to the positive control drug dexamethasone.