Bisphosphonated Benzoxazinorifamycin Prodrugs for the Prevention and Treatment of Osteomyelitis
ChemMedChem2008Vol. 3(12), pp. 1863–1868
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Ranga Reddy, Evelyne Dietrich, Yanick Lafontaine, Tom J. Houghton, Odette Bélanger, Anik Dubois, Francis F. Arhin, Ingrid Sarmiento, Ibtihal Fadhil, Karine Laquerre, Valérie Ostiguy, Dario Lehoux, Greg Moeck, Thomas Parr, Adel Rafai Far
Abstract
Benzoxazinorifamycins are potent antibacterial agents currently in development. Tethering these antibiotics to a bisphosphonate functional group by a cleavable linker allows the delivery of these agents to osseous tissues, where they can be released over time to treat bone infections. Various linker strategies are presented herein to develop osteotropic prodrugs, the activities of which are examined in vitro and in vivo.
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