亲脂性 N-酰基二胺的结构与抗菌活性的关系。
Relationship between structure and antibacterial activity of lipophilic N-acyldiamines.
机构信息
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, 36036-900 Juiz de Fora, MG, Brazil.
出版信息
Biomed Pharmacother. 2010 Apr;64(4):287-90. doi: 10.1016/j.biopha.2009.09.013. Epub 2009 Nov 5.
We report in this work the preparation and antibacterial evaluation of a series of N-monoacylated diamines against six Gram-positive and 11 Gram-negative bacteria. The results obtained showed the existence of relationship between lipophilicity and antibacterial activity of the tested compounds. The best results were obtained against Gram-positive bacteria for compounds having a 10-12 carbons alkyl chain. Compound 4e was the most active against Microccus lentus (MIC=2 microg/mL), Staphylococcus aureus ATCC 29213 (MIC=4 microg/mL) and Enterobacter aerogenes CDC 1680 (MIC=8 microg/mL).
在这项工作中，我们报告了一系列 N-单酰化二胺的制备和抗菌评价，这些二胺针对六种革兰氏阳性菌和 11 种革兰氏阴性菌。结果表明，所测试化合物的亲脂性与抗菌活性之间存在关系。对于具有 10-12 个碳原子烷基链的化合物，在对抗革兰氏阳性菌方面取得了最佳效果。化合物 4e 对微球菌 lentus（MIC=2μg/mL）、金黄色葡萄球菌 ATCC 29213（MIC=4μg/mL）和产气肠杆菌 CDC 1680（MIC=8μg/mL）的活性最强。
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