| 唐燕玲,刘蓓,杨小碧,付丽琼,高慧,毛泽伟.化学通报,2019,82(10):942-945. |
| 3-芳基-5-噻吩基二氢吡唑磺胺衍生物的合成及其抗炎活性研究 |
| Synthesis and in vitro anti-inflammatory activity of 3-aryl-5-thienyl dihydropyrazole sulfonamide derivatives |
| 投稿时间：2019-06-16 修订日期：2019-06-25 |
| DOI： |
| 中文关键词: 二氢吡唑 磺胺 抗炎活性 |
| 英文关键词:dihydropyrazole sulfonamide derivatives anti-inflammatory activity |
| 基金项目:国家自然科学基金(81560620)，云南省科学技术厅-云南中医药大学应用基础研究联合专项（2017FF117 (-023)），云南中医药大学大学生创新创业训练计划项目（2018006） |
|
| 摘要点击次数: 1632 |
| 全文下载次数: 1 |
| 中文摘要: |
| 二氢吡唑是一类含有多种生物活性的五元氮杂环化合物,广泛存在于各种活性天然产物结构中。4-氟苯乙酮和N-甲基哌嗪经取代反应后,再与2-噻吩甲醛发生羟醛缩合生成哌嗪取代噻吩查尔酮(2)。化合物2与水合肼环化得到中间体化合物3,最后经磺酰氯衍生化,合成得到8个未见报道的3-芳基-5-噻吩基二氢吡唑磺胺衍生物(4a-4h),其结构均经IR、1H NMR和13C NMR确证。采用小鼠巨噬细胞Raw264.7模型初步测试了衍生物的抗炎活性,结果表明,化合物4a、4e和4h具有潜在的体外抗炎活性,特别是化合物4a抑制NO生成的IC50值为12.64 μM,与阳性对照药地塞米松活性相当。 |
| 英文摘要: |
| Dihydropyrazole is an important five-membered N-heterocyclic compound with a broad range of biological activities, which widely exist in various active natural products. In this study, eight new 3-aryl-5-(2-thienyl)-4, 5-dihydro-1H-pyrazole derivatives (4a-4h) have been prepared, and their in vitro anti-inflammatory activities have been tested by lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages. The structures of title compounds were characterized by IR, 1H NMR and 13C NMR. The biological results indicated that the sulfonamide derivatives 4a, 4e and 4h displayed potential anti-inflammatory activity. Especially compound 4a had the most inhibitory effect on NO generation (IC50=12.64 μM), which was considered as lead compounds for further research. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |
|
|
|