中文关键词:二氢吡唑磺胺抗炎活性 英文关键词:dihydropyrazolesulfonamide derivativesanti-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）

作者	单位	E-mail
唐燕玲	云南中医药大学中药学院	m18487302692@163.com
刘蓓	云南中医药大学中药学院
杨小碧	云南中医药大学中药学院
付丽琼	云南中医药大学中药学院
高慧	云南中医药大学中药学院
毛泽伟	云南中医药大学中药学院	ydmason@163.com

摘要点击次数:1156 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 相关附件：部分化合物谱图.docx版权转让声明书附件1附件2 -->