Synthesis of osteotropic hydroxybisphosphonate derivatives of fluoroquinolone antibacterials.

  title={Synthesis of osteotropic hydroxybisphosphonate derivatives of fluoroquinolone antibacterials.},
  author={J. Mcpherson and R. Runner and T. Buxton and J. Hartmann and D. Fǎrcaşiu and Ilona Bereczki and E. Rőth and Szilvia Tollas and E. Ostorh{\'a}zi and F. Rozgonyi and P. Herczegh},
  journal={European journal of medicinal chemistry},
  volume={47 1},
  • J. Mcpherson, R. Runner, +8 authors P. Herczegh
  • Published 2012
  • Chemistry, Medicine
  • European journal of medicinal chemistry
  • 1-Hydroxybisphosphonate derivatives of ciprofloxacin, gatifloxacin and moxifloxacin have been synthesized using Cu(I) catalyzed azide-alkyne 1,3-dipolar cycloaddition reaction. The 1,2,3-triazol linked hydroxybisphosphonate derivative of ciprofloxacin exhibited antibacterial activity comparable to the parent antibiotic and all fluoroquinolone-bisphosphonates displayed osteotropic properties in a bone model. 
    39 Citations
    Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates.
    • 23
    • PDF
    Modifications of quinolones and fluoroquinolones: hybrid compounds and dual-action molecules
    • 18
    • PDF


    Osteoadsorptive bisphosphonate derivatives of fluoroquinolone antibacterials.
    • 56
    Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
    • 34
    The pharmacology of bisphosphonates and new insights into their mechanisms of action
    • R. Russell, M. Rogers, +6 authors H. A. Fleisch
    • Chemistry, Medicine
    • Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research
    • 1999
    • 254
    Bisphosphonates as a foundation of drug delivery to bone.
    • H. Uludağ
    • Medicine
    • Current pharmaceutical design
    • 2002
    • 94
    Bisphosphonates: a review of their pharmacokinetic properties.
    • J. Lin
    • Chemistry, Medicine
    • Bone
    • 1996
    • 773
    Bisphosphonates: preclinical aspects and use in osteoporosis.
    • 219