Osteoadsorptive bisphosphonate derivatives of fluoroquinolone antibacterials

Pál Herczegh, Thomas B. Buxton, James C. McPherson, Árpád Kovács-Kulyassa, Phyllis D. Brewer, Ferenc Sztaricskai, Gary G. Stroebel, Kent M. Plowman, Dan Farcasiu, John F. Hartmann

Research output: Contribution to journalArticle

65 Scopus citations

Abstract

Bisphosphonates conjugated to fluoroquinolone antibacterials through an intermediate carbon had better activity than conjugates lacking the carbon. Virtually all molar-based activity of these esterified bisphosphonate derivatives was identical to that of its parent. De-esterified free-acid forms retained good activity against most Gram-negative bacteria, but not against Gram-positives. A free-acid derivative remained bound to washed bone and completely inhibited Staphylococcus aureus growth. The more potent parent, ciprofloxacin, failed to bind significantly, and bacterial growth occurred.

Original languageEnglish (US)
Pages (from-to)2338-2341
Number of pages4
JournalJournal of Medicinal Chemistry
Volume45
Issue number11
DOIs
StatePublished - May 23 2002

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Herczegh, P., Buxton, T. B., McPherson, J. C., Kovács-Kulyassa, Á., Brewer, P. D., Sztaricskai, F., Stroebel, G. G., Plowman, K. M., Farcasiu, D., & Hartmann, J. F. (2002). Osteoadsorptive bisphosphonate derivatives of fluoroquinolone antibacterials. Journal of Medicinal Chemistry, 45(11), 2338-2341. https://doi.org/10.1021/jm0105326