School of Pharmacy and Biomolecular Sciences, Liverpool John Moores University, Byrom Street, Liverpool L3 3AF, UK.
Int J Antimicrob Agents. 2010 Apr;35(4):405-9. doi: 10.1016/j.ijantimicag.2009.11.022. Epub 2010 Jan 8.
Synthesis and antibacterial screening of a homologous series of 3-dialkylaminophenothiazinium-7-norfloxacin conjugates was carried out alongside a corresponding series of symmetrical methylene blue derivatives. The norfloxacin conjugates maintained typical methylene blue derivative photoproperties, such as long wavelength absorption, but produced no measurable singlet oxygen in the standard assay and provided no significant increase in the magnitude of photoantibacterial action, this being similar to the methylene blue homologues, although both the conjugates and homologues were considerably more active than methylene blue itself both against Staphylococcus aureus and Escherichia coli. DNA binding via intercalation was considerably greater for the series of norfloxacin conjugates than for the methylene blue homologues.
合成并筛选了一系列 3-二烷基氨基吩噻嗪-7-诺氟沙星缀合物以及相应的一系列对称亚甲蓝衍生物。这些诺氟沙星缀合物保持了典型的亚甲蓝衍生物的光物理性质，如长波长吸收，但在标准测定中没有产生可测量的单线态氧，也没有显著增加光抗菌作用的幅度，这与亚甲蓝类似，尽管这些缀合物和类似物都比亚甲蓝本身对金黄色葡萄球菌和大肠杆菌更具活性。通过嵌入与 DNA 的结合对于诺氟沙星缀合物系列而言要大大强于亚甲蓝类似物。
