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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Synthesis and biological evaluation of new l,3,4thiadiazepino7,6-bquinolin-2-amines as potent anti-microbial agents
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Synthesis and biological evaluation of new l,3,4thiadiazepino7,6-bquinolin-2-amines as potent anti-microbial agents

机译：新型l，3,4噻二氮卓并7,6-b喹啉-2-胺作为有效抗菌剂的合成和生物学评价

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摘要

Four series of 56 new thiadiazepinoquinoline amines were synthesized and characterized by spectro-scopic techniques (NMR, IR, and MS) and elemental analysis. All the compounds were screened for in vitro antimicrobial activity. Highest inhibitory activity (MIC of 0.03 mg/ml) was exerted by 2e against Bacillus subtilis and Streptococcus pyogenes, 2f against Escherichia coli and Streptococcus pyogenes, and 4k against only Bacillus subtilis. Only compounds 1g and 2g revealed potent anti-fungal activity (MIC 0.03 mg/ml) compared to the standard against Alternaria alternata. Most of the compounds exhibited better anti-bacterial activity than anti-fungal activity against the microorganisms employed in this study. These studies suggest that the thiadiazepinoquinoline scaffold may serve as a new promising template for further elaboration as anti-bacterial and anti-fungal drugs.
机译：合成了4个系列的56种新型噻二氮杂环喹啉胺，并通过光谱技术（NMR、IR和MS）和元素分析对其进行了表征。对所有化合物进行体外抗菌活性筛选。2e对枯草芽孢杆菌和化脓性链球菌，2f对大肠杆菌和化脓性链球菌，4k仅对枯草芽孢杆菌具有最高的抑制活性（MIC为0.03 mg/ml）。只有化合物 1g 和 2g 显示出有效的抗真菌活性 （MIC 0.03 mg/ml） 与链格孢菌的标准品相比。大多数化合物对本研究中使用的微生物表现出比抗真菌活性更好的抗菌活性。这些研究表明，噻二氮杂卓喹啉支架可以作为进一步阐述为抗菌和抗真菌药物的新的有前途的模板。

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