Biological activity against reference and multi-drug resistant (MDR) clinical strains of fluoroquinolones (FQs): ciprofloxacin (HCp), norfloxacin (HNr), lomefloxacin (HLm) and sparfloxacin (HSf), phosphine ligands derived from those antibiotics and 14 phosphino copper(I) and copper(II) complexes with 2,9-dimethyl-1,10-phenanthroline, 1,10-phenanthroline or 2,2′-biquinoline have been determined. Almost all phosphines showed excellent antibacterial activity relative to reference strains (S. aureus ATCC 6538, E. coli ATCC 25922, K. pneumoniae ATCC 4352, and P. aeruginosa ATCC 27853). In rare cases P. aeruginosa rods showed natural insensitivity to oxides, and their copper(II) complexes. Most of the studied compounds showed weak antibacterial activity against clinical multi-drug resistant strains (MDR P. aeruginosa 16, 46, 325, 355, MRD A. baumanii 483 and MDR S. aureus 177). However, phosphines Ph₂PCH₂Sf (PSf), Ph₂PCH₂Lm (PLm) and their copper(I) complexes were characterized by the best antibacterial activity. In addition, PSf compounds, in which the activities relative to P. aeruginosa MDRs were relatively diverse, paid particular attention in our studies. Genetic and phenotypic studies of these strains showed significant differences between the strains, indicating different profiles of FQs resistance mechanisms. This may prove that a change in the spatial conformation of the PSf derivatives relative to the native form of HSf increased its affinity for the target site of action in gyrase, leading to selective inhibition of the multiplication of MDR strains. In conclusion, differences in PSf activity within closely related P. aeruginosa strains may indicate its diagnostic and therapeutic potential.

对氟喹诺酮类（FQs）的参考和多重耐药（MDR）临床菌株的生物活性：环丙沙星（HCp），诺氟沙星（HNr），洛美沙星（HLm）和司巴沙星（HSf），源自这些铜和14膦的膦配体已确定（I）和铜（II）与2,9-二甲基-1,10-菲咯啉，1,10-菲咯啉或2,2'-联喹啉的配合物。相对于参考菌株（金黄色葡萄球菌ATCC 6538，大肠杆菌ATCC 25922，肺炎克雷伯氏菌ATCC 4352和铜绿假单胞菌ATCC 27853），几乎所有的膦都显示出优异的抗菌活性。在极少数情况下，铜绿假单胞菌棒对氧化物及其铜（II）配合物表现出天然不敏感性。大多数研究的化合物对临床多重耐药菌株（MDR铜绿假单胞菌16、46、325、355，MRDA鲍曼不动产483和MDR金黄色葡萄球菌177）显示出弱的抗菌活性。然而，膦Ph ₂ PCH ₂ Sf （PSf），Ph ₂ PCH ₂ Lm （PLm）及其铜（I）配合物具有最佳的抗菌活性。另外，PSf化合物，其中的活性相对于铜绿假单胞菌耐多药性相对多样，在我们的研究中特别注意。这些菌株的遗传和表型研究表明，这些菌株之间存在显着差异，表明FQs抗性机制的概况不同。这可证明的是，在的空间构象的变化的PSf相对于天然形式的衍生物HSF增加其亲和力在促旋酶作用的目标位点，导致MDR菌株的乘法的选择性抑制。总之，密切相关的铜绿假单胞菌菌株在PSf活性上的差异可能表明其诊断和治疗潜力。