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含均三唑环的新型联苯四唑衍生物的合成及抗菌活性

Synthesis and Antibacterial Activities of New Biphenyltetrazole Derivatives Bearing 1,2,4-Triazole

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【作者】 晁淑军惠新平李硕许鹏飞张自义王勤王燕玲

【Author】 CHAO, Shu-Juna HUI, Xin-Pinga LI, Shuoa XU, Peng-Fei*, a ZHANG, Zi-Yia WANG, Qinb WANG, Yan-Lingb (a State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000) (b College of Life Science, Lanzhou University, Lanzhou 730000)

【机构】 兰州大学功能有机分子化学国家重点实验室化学化工学院兰州大学生命科学学院兰州大学生命科学学院 兰州730000兰州730000兰州730000

【摘要】 通过4-芳基-5-(4-吡啶基)-1,2,4-三唑-3-硫醇(1)和2-三苯基甲基-5-(4′-溴甲基联苯-2-基)-四唑(5)反应,制得一系列新的S-烷基化产物(6),S-烷基化产物在酸性条件下脱保护,得到了14个未见文献报道的含1,2,4-三唑类联苯四唑(7a~7n)衍生物.结构经元素分析,IR,NMR及FAB-MS确认.对大肠杆菌、链球菌、枯草杆菌、金黄色葡萄球菌初步抑菌试验证明,多数化合物表现了较好的抑菌活性.

【Abstract】 S-Alkylation products were synthesized by the reaction of 4-aryl-5-(4-pridyl)-1,2,4-triazole-3- thiol (1) with 2-trityl-5-(4′-bromomethylbiphen-2-yl)tetrazole (5). An attempt to remove the trityl group of S-alkylation products 6 under acidic conditions gave fourteen new triazole ring containing biphenyl tetra- zoles 7a~7n in good yields. The structures of these compounds synthesized were confirmed by elemental analyses, IR, NMR and FAB-MS. Primary antibacterial test against E. coli, Streptococcus, B. subtilis and S. aureus showed that most of them had good antibacterial activities.

【基金】 国家自然科学基金(Nos.20021001,20372027);甘肃省中青年自然科学基金(No.YS-011-A25-001)资助项目.
  • 【文献出处】 化学学报 ,Acta Chimica Sinica , 编辑部邮箱 ,2005年06期
  • 【分类号】O626
  • 【被引频次】13
  • 【下载频次】387
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