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Bisphosphonated Benzoxazinorifamycin Prodrugs for the Prevention and Treatment of Osteomyelitis
Author(s) -
Reddy Ranga,
Dietrich Evelyne,
Lafontaine Yanick,
Houghton Tom J.,
Belanger Odette,
Dubois Anik,
Arhin Francis F.,
Sarmiento Ingrid,
Fadhil Ibtihal,
Laquerre Karine,
Ostiguy Valerie,
Lehoux Dario,
Moeck Gregory,
Parr Thomas R.,
Rafai Far Adel
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800255
Subject(s) - prodrug , osteomyelitis , medicine , pharmacology , intensive care medicine , surgery
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.