Recently, fluorenylmethyloxycarbonyl (Fmoc) conjugated amino acids (Fmoc-AA), especially Fmoc-phenylalanine (Fmoc-F), have been discovered to have antimicrobial properties specific to Gram-positive bacteria including MRSA. Their weak antibacterial activity against Gram-negative bacteria is due to their inability to cross the bacterial membrane. Here in order to increase the antibacterial spectrum of Fmoc-F, we prepared a formulation of Fmoc-F with the Gram-negative specific antibiotic aztreonam (AZT). This formulation displayed antibacterial activity against both Gram-positive and Gram-negative bacteria and significantly reduced the bacterial load in a mouse wound infection model. The combination produced a synergistic effect and higher efficacy against P. aeruginosa due to the increased Fmoc-F permeability by AZT through the bacterial membrane. This combinatorial approach could be an effective strategy for other Fmoc-AA having a Gram-positive specific antibacterial effect for the better management of bacterial wound infections.

中文翻译：

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Fmoc-苯丙氨酸水凝胶与氨曲南之间基于机制的抗菌协同作用的发展。

最近，已发现芴基甲氧基羰基（Fmoc）共轭氨基酸（Fmoc-AA），特别是Fmoc-苯丙氨酸（Fmoc-F）具有包括MRSA在内的革兰氏阳性细菌特有的抗菌特性。它们对革兰氏阴性细菌的弱抗菌活性是由于它们无法穿过细菌膜。在这里，为了增加Fmoc-F的抗菌谱，我们制备了具有革兰氏阴性特异性抗生素氨曲南（AZT）的Fmoc-F制剂。该制剂对革兰氏阳性菌和革兰氏阴性菌均显示出抗菌活性，并在小鼠伤口感染模型中显着降低了细菌载量。由于AZT通过细菌膜增加了Fmoc-F的通透性，因此该组合产生了对抗铜绿假单胞菌的协同作用和更高的功效。