哌嗪基连接的环丙沙星二聚体对耐甲氧西林金黄色葡萄球菌耐药菌株具有活性所需的结构特征。
Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus.
作者信息
Kerns Robert J, Rybak Michael J, Kaatz Glenn W, Vaka Flamur, Cha Raymond, Grucz Richard G, Diwadkar Veena U
机构信息
Division of Medicinal and Natural Products Chemistry, The University of Iowa, 52242, Iowa City, IA, USA.
出版信息
Bioorg Med Chem Lett. 2003 Jul 7;13(13):2109-12. doi: 10.1016/s0960-894x(03)00376-7.
We previously demonstrated that piperazinyl-linked fluoroquinolone dimers possess potent antibacterial activity against drug-resistant strains of Staphylococcus aureus. In this study, we report the preparation and evaluation of a series of incomplete dimers toward ascertaining structural features of piperazinyl-linked ciprofloxacin dimers that render these agents refractory to fluoroquinolone-resistance mechanisms in Staphylococcus aureus.
我们先前证明，哌嗪基连接的氟喹诺酮二聚体对耐甲氧西林金黄色葡萄球菌具有强大的抗菌活性。在本研究中，我们报告了一系列不完全二聚体的制备和评估，以确定哌嗪基连接的环丙沙星二聚体的结构特征，这些特征使这些药物对金黄色葡萄球菌中的氟喹诺酮耐药机制具有抗性。
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