双氨基三唑硫醚及其与胡椒醛席夫碱的合成及抗菌活性  

Syntheses and Antibacterial Activities of Bis(amino-triazole sulfurether) and Their Piperonal Schiff′s Base Derivatives

作　　者：胡国强[1] 谢松强[1] 杜刚军[1] 黄文龙[2] 张惠斌[2] 黄胜堂[2] 

机构地区：[1]河南大学药学院,开封475004 [2]中国药科大学新药中心

出　　处：《应用化学》2006年第3期273-277,共5页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金(30070861);河南大学科研基金(04ZDZR009)资助项目

摘　　要：氨基均三唑巯醇(1a^1n)与1,2-二溴乙烷缩合得双氨基三唑硫醚(2a^2n),再与胡椒醛缩合得相应的双席夫碱(3a^3n)。新化合物结构由IR、1H NMR、MS和元素分析测试技术确证。体外抗活性结果表明,在质量分数为0.01%的浓度下,胺类衍生物2c和2m对金黄色葡萄球菌、化合物2g对变形杆菌表现出了较强的抑制活性,而席夫碱衍生物除对大肠杆菌表现较强的抑制活性外,对金黄色葡萄球菌也表现出明显的抑菌活性。Bis（amino-triazole sulfurethers） （2a -2n） and the corresponding piperonal schiff＇s base derivatives（3a- 3n） were synthesized via the condensation of amino-triazole thiols（1a -1n） with 1,2-dibromoenthane to obtain 2a - 2n followed by the condensation of compounds 2a - 2n with piperonal in acetic acid, respectively. The compounds were confirmed by IR, ^1H NMR, MS and elemental analysis. Among the new compounds synthesized, the sulfurether compounds （2c）, （2m） exhibit strong inhibiting activity against Staphylococcus aureus, and compound 2g does against Proteus vtdgaris in dosage of 1.0 × 10^-4 （mass fraction） ; the schiff＇s base compounds 3a - 3j exhibit stronger inhibiting activity to Escherichia. coli, while they exhibit medium inhibiting activity to Staphylococcus aureus.

关 键 词：均三唑 硫醚 席夫碱 抗菌活性 

分 类 号：O621[理学—有机化学]