| 8-羟基喹啉衍生物作为潜在的艰难梭菌抗生素的设计、合成和活性评价 |
| 投稿时间：2023-03-10 修订日期：2023-10-03 点此下载全文 |
| 引用本文：叶腾飞,程涛,宋平,计伟莉,卞晓岚.8-羟基喹啉衍生物作为潜在的艰难梭菌抗生素的设计、合成和活性评价[J].药学实践杂志,2023,41(12):737~740 |
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| 中文摘要:目的 艰难梭菌感染（CDI）目前治疗措施主要包括抗生素疗法、粪菌移植疗法等，其治疗后存在较高的复发率，需寻求一种更有效的替代疗法。方法 本研究基于有前景的8-羟基喹啉骨架，设计、合成了一系列8-羟基喹啉衍生物。结果 针对艰难梭菌的活性测试表明，多数分子对艰难梭菌具有良好的抑菌作用，其中化合物 6f 显示出较强的杀伤艰难梭菌活性。结论 本研究发现了新型具有抗艰难梭菌的8-羟基喹啉衍生物，可作为良好的先导化合物进一步研发。 |
| 中文关键词:艰难梭菌 抗感染 8-羟基喹啉衍生物 构效关系 |
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| Design, synthesis and biological evaluation of 8-hydroxyquinoline derivatives as potential clostridium difficile antibiotics |
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| Abstract:Objective To find a more effective alternative therapy for antibiotic therapy and fecal microbiota transplantation in current primary treatment of clostridioides difficile infection (CDI) because of the high recurrence rate.Methods A series of 8-hydroxyquinoline derivatives were designed and synthesized based on 8-hydroxyquinoline scarffold. Results The activity test against C. difficile showed that most of the molecules exhibited good antibacterial activity against C. difficile, and compound 6f showed attractive anti-C. difficile activity. Conclusion A new type of 8-hydroxyquinoline derivatives with anti-clostridium difficile was found, which could be used as good lead compounds for further development. |
| keywords:clostridium difficile anti-infection 8-hydroxyquinoline derivatives structure-activity relationship |
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