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抗结核药物的合成及抗菌活性
引用本文:李 丽1,张 焕1,曾祥聪1,丁 娇1,马 峻2,祝 宏1. 抗结核药物的合成及抗菌活性[J]. 武汉工程大学学报, 2019, 0(6): 527-531
作者姓名:李 丽1  张 焕1  曾祥聪1  丁 娇1  马 峻2  祝 宏1
作者单位:1. 武汉工程大学化工与制药学院,湖北 武汉 430205;2. 武汉市金银潭医院,湖北 武汉 430023
摘    要:采用杂合的方法合成乙酰水杨酸-吡嗪酰胺和氧氟沙星-磺胺醋酰两个抗结核药物。通过红外光谱、核磁共振氢谱、核磁共振碳谱、质谱对它们的结构对进行了表征。采用肉汤稀释法测定这2个目标化合物对标准结核杆菌的最低抑菌质量浓度,结果表明:乙酰水杨酸-吡嗪酰胺的最低抑菌质量浓度为62.5 μg/mL,氧氟沙星-磺胺醋酰的最低抑菌质量浓度为125 μg/mL,证明其具有较好的抑菌活性。

关 键 词:抗结核药物  杂合  抑菌活性  乙酰水杨酸-吡嗪酰胺  氧氟沙星-磺胺醋酰

Synthesis and Antibacterial Activities of Anti-Tuberculosis Drugs
LI Li1,ZHANG Huan1,ZENG Xiangcong1,DING Jiao1,MA Jun2,ZHU Hong1. Synthesis and Antibacterial Activities of Anti-Tuberculosis Drugs[J]. Journal of Wuhan Institute of Chemical Technology, 2019, 0(6): 527-531
Authors:LI Li1  ZHANG Huan1  ZENG Xiangcong1  DING Jiao1  MA Jun2  ZHU Hong1
Affiliation:1. School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Wuhan 430205,China;2. Wuhan Jinyintan Hospital, Wuhan 430023, China
Abstract:Two hybrid anti-tuberculosis drugs of acetylsalicylic acid-pyrazineamide and ofloxacin- sulfacetamide were synthesized by hybrid strategy for better antibacterial performances. The structures were characterized by infrared spectroscopy, 1H nuclear magnetic resonance spectroscopy, 13C nuclear magnetic resonance spectroscopy and mass spectrometry. The minimum inhibitory mass concentrations of the two target drugs against standard tuberculosis were determined by broth dilution method. The results show that the minimum inhibitory mass concentration of acetylsalicylic acid-pyrazine is 62.5 μg/mL, while that of ofloxacin- sulfacetamide is 125 μg/ mL, suggesting that the drugs have good inhibitory activities.
Keywords:antituberculosis drugs  hybrid  antibacterial activity  acetylsalicylic acid-pyrazineamide  ofloxacin-sulfacetamide
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