化学
白色念珠菌
抗菌剂
青蒿琥酯
金黄色葡萄球菌
罗红霉素
微生物学
抗生素
有机化学
生物化学
细菌
免疫学
疟疾
恶性疟原虫
生物
红霉素
遗传学
作者
Sheng He,Xi‐Lin Ouyang,Xiaochao Huang,Weisong Hu,Weilong Dai,Xiaoyan Tian,Ying-Ming Pan,Shi‐Wen Huang,Heng‐Shan Wang
出处
期刊:Letters in Drug Design & Discovery
[Bentham Science]
日期:2015-03-24
卷期号:12 (5): 408-416
被引量:10
标识
DOI:10.2174/1570180812666141125004502
摘要
Thirteen α-aminophosphonate derivatives with artesunate were synthesized by introducing bioactive α-aminophosphonate combination with artesunate in this work. The reaction were easily carried out at normal pressure, low temperature and without any catalyst. Four strains of microbials, namely Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans, were used for the evaluation of the antimicrobial activities of these target compounds. Experimental results indicated that most of the compounds had good inhibitory effects. Compound 7k showed obvious antimicrobial activities with the MICs of 64 μg/ml against Staphylococcus aureus and 32 μg/ml against Candida albicans. Furthermore, when combined with roxithromycin, the synthesized compounds showed overlapping enhanced activities and proved potential antimicrobial synergists of roxithromycin. Keywords: Artesunate, α-aminophosphonate, Antimicrobial Activity, Synthesis.
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