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

作　　者：晁淑军[1] 惠新平[1] 李硕[1] 许鹏飞[1] 张自义[1] 王勤[2] 王燕玲[2] 

机构地区：[1]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730000 [2]兰州大学生命科学学院,兰州730000

出　　处：《化学学报》2005年第6期525-532,F009,共9页Acta Chimica Sinica

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.

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.S-Alkylation products were synthesized by the reaction of 4-aryl-5-(4-pridyl)-1,2,4-triazole-3thiol (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 tetrazoles 7a similar to 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.

关 键 词：S-烷基化 四唑 三唑 衍生物 联苯 新型 芳基 金黄色葡萄球菌 FAB 抗菌活性 

分 类 号：O626[理学—有机化学]