Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis

…, F Viens, FF Arhin, I Sarmiento, D Lehoux…

Index: Houghton, Tom J.; Tanaka, Kelly S. E.; Kang, Ting; Dietrich, Evelyne; Lafontaine, Yanick; Delorme, Daniel; Ferreira, Sandra S.; 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.; Far, Adel Rafai Journal of Medicinal Chemistry, 2008 , vol. 51, # 21 p. 6955 - 6969

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Citation Number: 27

Abstract

Osteomyelitis is an infection located in bone and a notoriously difficult disease to manage, requiring frequent and heavy doses of systemically administered antibiotics. Targeting antibiotics to the bone after systemic administration may provide both greater efficacy of treatment and less frequent administration. By taking advantage of the affinity of the bisphosphonate group for bone mineral, we have prepared a set of 13 bisphosphonated ...