| 黎勇坤,郑 喜,朱加洪,王 斯,杨林丽,毛泽伟.化学通报,2018,81(5):461-465. |
| 3-芳基-5-(2-呋喃基)-4, 5-二氢吡唑衍生物的合成及其生物活性评价 |
| Synthesis and biological evaluation of 3-aryl-5-(2-furanyl)-4, 5-dihydropyrazole derivatives |
| 投稿时间：2017-10-31 修订日期：2018-02-04 |
| DOI： |
| 中文关键词: 二氢吡唑衍生物 抗炎活性 抗氧化活性 |
| 英文关键词:dihydropyrazole derivatives anti-inflammatory activity antioxidant activity |
| 基金项目:云南省科学技术厅-云南中医学院应用基础研究联合专项(2017FF117 (-023)) |
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| 中文摘要: |
| 二氢吡唑类化合物是一类具有良好生物活性的五元杂环化合物。本文以2-呋喃甲醛和4-氟苯乙酮为原料,经羟醛缩合和取代反应生成4’-二甲氨基呋喃查尔酮(2)后,与水合肼环化得到二氢吡唑中间体(3),再酰化得到9个未见报道的5-(2-呋喃基)-3-芳基-4, 5-二氢-1H-吡唑衍生物(4a-4i),其结构经IR、1H NMR和13C NMR确证。分别采用小鼠巨噬细胞Raw264.7模型和DHHP法初步测试了目标化合物的体外抗炎活性和抗氧化活性,结果表明,部分化合物具有潜在的抗炎活性和清除自由基活性,特别是化合物4b和4c的抗炎活性与阳性对照药地塞米松活性相当(IC50值分别为7.84μM和10.52μM),而化合物3、4b、4c和4d在浓度为4mg/mL时对DPPH自由基的清除率均超过90%。 |
| 英文摘要: |
| Dihydropyrazole, a five-membered heterocyclic molecule, is an important organic compound with a broad range of biological activities. In this study, nine new 3-aryl-5-(2-furanyl)-4, 5-dihydro-1H-pyrazole derivatives have been synthesized, and their in vitro anti-inflammatory and antioxidant activities were evaluated in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and DPPH model, respectively. The structures were characterized by IR, 1H NMR and 13C NMR. The biological results demonstrated that the amide compounds showed potential anti-inflammatory and antioxidant activity. In particular, compound 4b and 4c were found to be similar anti-inflammatory to positive control dexamethasone (IC50=7.84 μM and 10.52 μM, respectively), and DPPH free radical scavenging rate of compound 3, 4b, 4c and 4d was up to 90% (4 mg/mL). |
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