PMID- 16466892 OWN - NLM STAT- MEDLINE DCOM- 20060609 LR - 20131121 IS - 0732-8893 (Print) IS - 0732-8893 (Linking) VI - 54 IP - 4 DP - 2006 Apr TI - Susceptibility studies of piperazinyl-cross-linked fluoroquinolone dimers against test strains of Gram-positive and Gram-negative bacteria. PG - 305-10 AB - Susceptibility testing was used to evaluate potential spectrum of action for piperazinyl-cross-linked fluoroquinolone dimers against test strains of Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, Mycobacterium tuberculosis, and vancomycin-resistant Enterococcus faecium (VRE) and to evaluate dimers against fluoroquinolone-resistant and fluoroquinolone-susceptible strains of streptococci. Individual dimers displayed equivalent or lowered MIC values compared with parent fluoroquinolone monomers against test strains of S. pneumoniae, S. pyogenes, E. coli, and VRE. Raised MIC values were observed for all dimers in comparison to monomers against test strains of P. aeruginosa and E. coli. In comparison to parent fluoroquinolones, all dimers displayed decreased percent inhibition of growth against M. tuberculosis. Structural requirements for activity of dimers and partial dimers against all organisms, including lower MICs against certain fluoroquinolone-resistant and fluoroquinolone-susceptible strains of streptococci, were consistent with requirements previously observed for dimers against fluoroquinolone-susceptible and fluoroquinolone-resistant strains of S. aureus. In contrast, the 10- to 100-fold lowering of MICs against wild-type and fluoroquinolone-resistant strains of S. aureus previously observed for individual cross-linked dimers was not observed with test strains of the various organisms used here. FAU - Kerns, Robert J AU - Kerns RJ AD - Division of Medicinal and Natural Products Chemistry, The University of Iowa, Iowa City, IA 52242-1112, USA. robert-kerns@uiowa.edu FAU - Rybak, Michael J AU - Rybak MJ FAU - Cheung, Chrissy M AU - Cheung CM LA - eng PT - Journal Article PT - Research Support, N.I.H., Extramural DEP - 20060208 PL - United States TA - Diagn Microbiol Infect Dis JT - Diagnostic microbiology and infectious disease JID - 8305899 RN - 0 (Fluoroquinolones) RN - 5E8K9I0O4U (Ciprofloxacin) RN - N0F8P22L1P (Norfloxacin) SB - IM MH - Ciprofloxacin/*analogs & derivatives MH - Dimerization MH - Drug Resistance, Bacterial MH - Fluoroquinolones/*chemistry/*pharmacology MH - Gram-Negative Bacteria/*drug effects MH - Gram-Positive Bacteria/*drug effects MH - Microbial Sensitivity Tests MH - Norfloxacin/*analogs & derivatives EDAT- 2006/02/10 09:00 MHDA- 2006/06/10 09:00 CRDT- 2006/02/10 09:00 PHST- 2005/08/03 00:00 [received] PHST- 2005/11/22 00:00 [revised] PHST- 2005/11/29 00:00 [accepted] PHST- 2006/02/10 09:00 [pubmed] PHST- 2006/06/10 09:00 [medline] PHST- 2006/02/10 09:00 [entrez] AID - S0732-8893(05)00340-8 [pii] AID - 10.1016/j.diagmicrobio.2005.11.004 [doi] PST - ppublish SO - Diagn Microbiol Infect Dis. 2006 Apr;54(4):305-10. doi: 10.1016/j.diagmicrobio.2005.11.004. Epub 2006 Feb 8.