Osteoadsorptive Bisphosphonate Derivatives of Fluoroquinolone Antibacterials

Autor: Herczegh, P., Buxton, T. B., McPherson, J. C., III, Kovacs-Kulyassa, A., Brewer, P. D., Sztaricskai, F., Stroebel, G. G., Plowman, K. M., Farcasiu, D., Hartmann, J. F.
Zdroj: Journal of Medicinal Chemistry; May 2002, Vol. 45 Issue: 11 p2338-2341, 4p
Abstrakt: 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.
Databáze: Supplemental Index