Osteoadsorptive bisphosphonate derivatives of fluoroquinolone antibacterials

被引:78
|
作者
Herczegh, P
Buxton, TB
McPherson, JC
Kovács-Kulyassa, A
Brewer, PD
Sztaricskai, F
Stroebel, GG
Plowman, KM
Farcasiu, D
Hartmann, JF
机构
[1] ElizaNor Biopharmaceut Inc, Princeton Jct, NJ 08550 USA
[2] Univ Debrecen, Hungarian Acad Sci, Res Grp Antibiot, Debrecen, Hungary
[3] Eisenhower Army Med Ctr, Dept Clin Invest, Ft Gordon, GA USA
[4] Augusta State Univ, Augusta, GA USA
关键词
D O I
10.1021/jm0105326
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:2338 / 2341
页数:4
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