| 张政,郑卫,李银萍,等.基于海洋天然产物oroidin的结构修饰及其衍生物的抑菌活性研究[J].中国海洋药物,2023,42(3):49-56. |
| 基于海洋天然产物oroidin的结构修饰及其衍生物的抑菌活性研究 |
| Structural modification based on marine natural product oroidin and antibacterial activity of its derivatives |
| 投稿时间：2022-03-14 修订日期：2022-04-08 |
| DOI：10.13400/j.cnki.cjmd.2023.03.008 |
| 中文关键词: 海洋天然产物 抑菌活性 乳清群海绵定 |
| English Keywords:marine natural products, antibacterial activity, oroidin |
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| 中文摘要: |
| 目的 针对海洋天然产物oroidin进行衍生物的合成以及抑菌活性评价。 方法 以吡咯-2-羧酸为起始原料，经过卤素取代、酰胺缩合、还原胺化等反应，四步合成oroidin类似物，并对衍生物进行抑菌活性评价。 结果 总计合成了20个衍生物，通过抑菌活性测试，发现了对多种菌株如枯草芽孢杆菌、草分枝杆菌、大肠杆菌等有抑制活性的化合物，其中化合物21和24对枯草芽孢杆菌的MIC值都达到3.125 μmol?L?1。该类化合物可应用于抗菌药物的开发。 |
| English Summary: |
| Objective To synthesize derivatives of marine natural product oroidin and evaluate their antibacterial activity. Methods Oroidin analogues were synthesized from pyrrole-2- carboxylic acid in four steps, including halogen substitution, amide condensation and reductive amination. The antibacterial activity of oroidin derivatives were tested. Results 20 derivatives were synthesized. The antibacterial activity of compounds 21 and 24 against Bacillus subtilis, Mycobacterium Phlei and Escherichia coli were tested. The MIC value of compounds 21 and 24 against Bacillus subtilis were 3.125 μmol?L?1. These compounds can be used in the development of antibacterial drugs. |
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