合成2-6-替代诺林-4-) -1-氧二醇作为潜在的抗菌菌剂
Abhijit Shinde1, Prashant P Thakare1, Yogesh Nandurkar1,2
1Department of Chemistry, S. P. Mandali's Sir Parashurambhau College (Affiliated to, Savitribai Phule Pune University), Tilak Road, Pune, 411030 India.
Chemicke zvesti
|May 30, 2023
概括
新的奇诺林衍生物显示出对抗耐药结核病的前景. 研究人员合成并测试了抗菌菌和抗菌活性的化合物,发现了几个具有强效和低毒性的化合物,为新的结核病治疗提供了希望.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 微生物学 微生物学
背景情况:
- 抗生素耐药性对全球健康构成重大威胁,特别是来自诸如结核病之类的真菌细菌感染.
- 迫切需要新型治疗药物来对抗耐药性结核菌菌株.
研究的目的:
- 合成和评估一系列新型的2 - 6 - 6 - 替代氨酸 - 4 - ) - 1 - 氧二醇衍生物的抗菌,抗菌和抗真菌活性.
- 确定强效和安全的化合物,用于开发新的抗感染药物.
主要方法:
- 合成2 - 6 - 替代的诺林 - 4 - ) - 1 - 氧二醇衍生物 (化合物8a - p).
- 使用光谱分析进行结构性表征.
- 在体外对抗 Mycobacterium tuberculosis H37Rv. 的抗结核活性进行了评估.
- 对抗Proteus mirabilis,大肠杆菌,细菌 Bacillus subtilis 和 Staphylococcus albus 的抗菌活性的评估.
- 对Candida albicans和Aspergillus niger的抗真菌活性进行查.
- 对L929小鼠纤维细胞的细胞毒性评估.
主要成果:
- 13种衍生品 (8a-m) 显示出中度到良好的抗结核活性 (MIC 9.2-106.4 μM).
- 化合物8a和8h的活性与pyrazinamide相当.
- 一些化合物显示出对葡萄球菌 (8c, 8d, 8e, 8g, 8k, 8o),Proteus mirabilis (8c) 和大肠杆菌 (8n) 的良好活性.
- 活性化合物对L929小鼠纤维细胞细胞没有显著的细胞毒性.
结论:
- 合成的2 - 6 - 6 - 替代的诺林 - 4 - 伊尔 - 1 - 氧二醇衍生物具有显著的抗菌和抗菌潜力.
- 化合物8a和8h是作为抗结核剂进一步开发的有希望的候选物.
- 活性化合物的低细胞毒性表明,潜在的治疗应用具有有利的安全性.
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