925684-17-9Relevant academic research and scientific papers
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis
Tanaka, Kelly S.E.,Houghton, Tom J.,Kang, Ting,Dietrich, Evelyne,Delorme, Daniel,Ferreira, Sandra S.,Caron, Laurence,Viens, Frederic,Arhin, Francis F.,Sarmiento, Ingrid,Lehoux, Dario,Fadhil, Ibtihal,Laquerre, Karine,Liu, Jing,Ostiguy, Valerie,Poirier, Hugo,Moeck, Gregory,Parr Jr., Thomas R.,Rafai Far, Adel
experimental part, p. 9217 - 9229 (2009/04/11)
Osteomyelitis is a difficult to treat bacterial infection of the bone. Delivering antibacterial agents to the bone may overcome the difficulties in treating this illness by effectively concentrating the antibiotic at the site of infection and by limiting the toxicity that may result from systemic exposure to the large doses conventionally used. Using bisphosphonates as osteophilic functional groups, different forms of fluoroquinolone esters were synthesized and evaluated for their ability to bind bone and to release the parent antibacterial agent. Bisphosphonated glycolamide fluoroquinolone esters were found to present a profile consistent with effective and rapid bone binding and efficient release of the active drug moiety. They were assessed for their ability to prevent bone infection in vivo and were found to be effective when the free fluoroquinolones were not.
Phosphonated Fluoroquinolones, Antibacterial Analogs Thereof, and Methods for the Prevention and Treatment of Bone and Joint Infections
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Page/Page column 75, (2008/12/09)
The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis.
