| 摘要: |
| 针对日益突出的结核病（TB）药物耐药性问题，对抗结核药物进行了合理的修饰，以增强其结核病治疗的效果.以异烟肼（INH）为原料，与不同的异氰酸酯反应，成功制备了9种新型的不对称取代脲类化合物，这类脲桥结构对结核分枝杆菌（MTB）中的半胱氨酸合酶具有抑制作用，合成的产物经质谱（MS）、氢核磁共振谱（1H NMR）等方法进行了分析表征. |
| 关键词: 抗结核 半胱氨酸合酶 脲桥 合成 |
| DOI：10.3969/J.ISSN.1000-5137.2020.04.007 |
| 分类号:O625.67 |
| 基金项目:国家自然科学基金（U1803282） |
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| Design and synthesis of antituberculosis compounds |
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ZOU Shun1, DUAN Liping2, XU Dongfang1, SUN Dazhi1
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1.College of Chemistry and Materials Science, Shanghai Normal University, Shanghai 200234, China;2.National Institute of Parasitic Diseases, Chinese Center for Disease Control and Prevention, Shanghai 200025, China
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| Abstract: |
| In view of the increasingly prominent drug resistance of tuberculosis(TB)drugs, the rational structure modification of antituberculosis drugs can improve the efficacy of TB treatment. In this paper, nine novel asymmetric substituted ureas were successfully prepared by reacting isoniazid(INH)with different isocyanates. This kind of urea bridge structure has inhibitory effect on cystine synthase in mycobacterium tuberculosis(MTB).The synthesized products were confirmed by mass spectrometry (MS)and nuclear magnetic resonance spectroscopy(1H NMR). |
| Key words: antituberculosis cysteine synthase urea bridge synthesis |
