| 高 慧,郑 喜,王 斯,杨林丽,毛泽伟.化学通报,2017,80(10):976-979. |
| 含酰基哌嗪片段的呋喃查尔酮衍生物的合成及其抗炎活性研究 |
| Studies on the synthesis and anti-inflammatory evaluation of acylpiperazine substituted furanyl chalcone derivatives |
| 投稿时间：2017-04-07 修订日期：2017-06-26 |
| DOI： |
| 中文关键词: 呋喃查尔酮衍生物 合成 抗炎活性 |
| 英文关键词:furanyl chalcone derivatives synthesis anti-inflammatory activity |
| 基金项目:国家自然科学基金项目（81560620）；云南省应用基础研究项目（2014FZ078, 2014FZ087） |
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| 中文摘要: |
| 依据活性结构单元的拼合原理，以2-呋喃甲醛和2-溴-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13C NMR确证。采用小鼠巨噬细胞Raw264.7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(IC50=3.88μM)，与阳性对照药地塞米松活性相当。 |
| 英文摘要: |
| A series of new 4’-(N-substitued-1-piperazinyl) furanyl chalcone derivatives have been synthesized, and their anti-inflammatory activities in vitro were evaluated in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages. The structures were characterized by 1H NMR and 13C NMR. The biological results demonstrated that sulfamide compounds showed higher anti-inflammatory activity than amides. In particular, compound 4d was found to be the most potent anti-inflammatory compound (IC50=3.88 μM), which was similar to positive control dexamethasone. |
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