Design, synthesis and biological evaluation of monobactams as antibacterial agents against gram-negative bacteria
Design, synthesis and biological evaluation of monobactams as antibacterial agents against gram-negative bacteria
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DOI：
10.1016/j.ejmech.2016.01.024
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发表时间：
2016-03-03
影响因子：
6.7
通讯作者：
Song, Dan-Qing
中科院分区：
文献类型：
--
作者：
Fu, Hai-Gen;Hu, Xin-Xin;Song, Dan-Qing
以氨曲南和BAL30072为先导化合物，制备了一系列单菌素类化合物，并对其对革兰氏阴性菌敏感和耐药菌株的抗菌活性进行了评价。基于特洛伊木马策略，合成了6个含有PIH类铁载体的偶联物(12a-f)，以增强对革兰氏阴性菌的杀菌活性，并对敏感的革兰氏阴性菌显示出较强的MIC活性
A series of monobactam derivatives were prepared and evaluated for their antibacterial activities against susceptible and resistant Gram-negative strains, taking Aztreonam and BAL30072 as the leads. Six conjugates (12a-f) bearing PIH-like siderophore moieties were created to enhance the bactericidal activities against Gram-negative bacteria based on Trojan Horse strategy, and all of them displayed potencies against susceptible Gram-negative strains with MIC