Document Report Card

ID: ALA1135427

Journal: J Med Chem

Title: Osteoadsorptive bisphosphonate derivatives of fluoroquinolone antibacterials.

Authors: Herczegh P, Buxton TB, McPherson JC, Kovács-Kulyassa A, Brewer PD, Sztaricskai F, Stroebel GG, Plowman KM, Farcasiu D, Hartmann JF.

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.

CiteXplore: 12014972

DOI: 10.1021/jm0105326