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Antibacterial agent 128
MCE 国际站：Antibacterial agent 128
产品活性：Antibacterial agent 128 是一种带有可裂解接头的铁载体类似物-环丙沙星 (Ciprofloxacin (Ciprofloxacin (HY-B0356))) 偶联物。Antibacterial agent 128 显示出针对铜绿假单胞菌 (MIC 值为 0.25-64 μg/mL) 和类鼻疽伯克氏菌 (MIC 值为 1-32 μg/mL) 的抗生素活性。
研究领域：Anti-infection
作用靶点：Bacterial | Antibiotic
In Vitro: Antibacterial agent 128 (compound 2d), bearing an hydroxypyridinone moiety with a cleavable linker, active on a large panel of strains of P. aeruginosa (MIC = 0.25-64 μg/mL), B. pseudomallei (MIC = 1-32 μg/mL) and B. thailandensis (MIC = 4-128 μg/mL). Moreover, Antibacterial agent 128 is active on the P. aeruginosa Ciprofloxacin-resistant strain AM85 without cytotoxicity.
Using iron transport systems is a promising strategy to bypass the bacteria cell membrane and restore the activity of conventional antibiotics such as Ciprofloxacin. The siderophore analogs correspond to a mono-catechol or a hydroxypyridinone moiety recognized by both Pseudomonas and Burkholderia species. Physico-chemical studies show that (i) conjugates were unable to interact or cross the membrane by passive diffusion and (ii) conjugates with cleavable linker are stable in physiologic environment.
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文献和实验Genomic Approaches to Antibacterial Discovery
of concept in curing experimental infections. The second approach is based on screening for compounds with antibacterial activity and then employing a broad variety of newer technologies to identify the molecular target of the antibacterial agent
Methods to Assay Inhibitors of tRNA Synthetase Activity
could be a potential antibacterial agent. Only one aa-RS inhibitor, the Ile-RS inhibitor mupirocin, is currently marketed as an antibacterial agent. We focused on phenylalanyl (Phe)-tRNA synthetase (Phe-RS), but the described methods are not restricted to Phe-RS
Assessing the Activity of Bacterial Multidrug Efflux Pumps
Resistance to antibiotics in target bacterial populations has long complicated antibacterial chemotherapy. First described in the early 1980s (1 , 2 ), efflux mechanism of resistance, whereby the antibiotic is actively (i.e., in an energy
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