文章摘要
李芳耀.1, 2, 3-三唑类磺胺的合成及抗菌活性[J].精细化工,2018,35(12):0
1, 2, 3-三唑类磺胺的合成及抗菌活性
Synthesis and Antibacterial Activities of Sulfonamides Derivatives Bearing 1, 2, 3-Triazole Moiety
投稿时间:2018-03-24  修订日期:2018-07-23
DOI:
中文关键词: 磺胺  三唑  合成  抗菌活性
英文关键词: sulfonamides  triazole  synthesis  antibacterial activity
基金项目:广西自然科学基金项目(2015GXNSFAA139035, 2016GXNSFAA380323),广西自然科学基金重大项目(2016GXNSFEA380001),国家级大学生创新创业训练计划项目(201510601020),桂林市科学研究与技术开发计划重点项目
作者单位E-mail
李芳耀 桂林医学院 lifangyao2006@163.com 
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中文摘要:
      以磺胺(4-氨基苯磺酰胺)为原料,其与氯乙酰氯反应得到中间体2-氯-N-(4-氨磺酰基苯基)乙酰胺(Ⅱ),然后(Ⅱ)与叠氮钠和端基炔“一锅法”反应合成了10个1, 2, 3-三唑类磺胺化合物(Ⅲa~Ⅲj),利用FTIR、1H NMR、13C NMR和ESI-MS对产物结构进行表征。采用二倍稀释法测定目标化合物的抗菌活性,结果表明:产物对金黄色葡萄球菌和大肠杆菌表现出一定的抗菌活性,特别是2-(4-(3-氟苯基)-1H-1, 2, 3-三唑-1-基)-N-(4-氨磺酰基苯基)乙酰胺(Ⅲh)对大肠杆菌的的MIC为0.25 μg/mL,与阳性对照药环丙沙星相当。
英文摘要:
      The Intermediate 2-chloro-N-(4-sulfamoylphenyl)acetamide(II) was obtained by the reaction of sulfanilamide and chloroacetyl chloride. Ten 1, 2, 3-triazolyl sulfonamides were prepared using a known one-pot procedure starting from (II), sodium azide and terminal alkynes. The target compounds were characterized by FTIR, 1H NMR, 13C NMR and ESI-MS. The minimal inhibitory concentrations (MIC) of target compounds against S.aureus and E.coli were determined with double broth dilution method. The results showed that all the tested compounds exhibited a certain antibacterial activities. In particular, 2-(4-(3-fluorophenyl)-1H-1, 2, 3-triazol-1- yl)-N-(4- sulfamoylphenyl)acetamide (IIIh) possessed similar activity against E.coli compared with the positive control drug (ciprofloxacin 0.25 μg/mL).
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