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 derivativesanti-inflammatory activityantioxidant 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))

作者	单位	E-mail
黎勇坤	云南中医学院中药学院	2537569119@qq.com
郑 喜	云南中医学院第一附属医院中心实验室
朱加洪	云南中医学院中药学院
王 斯	云南中医学院中药学院
杨林丽	云南中医学院中药学院
毛泽伟	云南中医学院中药学院	ydmason@163.com

摘要点击次数:1495 全文下载次数:0 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). 查看全文查看/发表评论下载PDF阅读器 相关附件：化合物谱图版权转让声明书修改说明 -->