Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis

作者：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 Thomas R Jr; Far Adel Rafai^*

来源：Bioorganic & Medicinal Chemistry, 2008, 16(20): 9217-9229.

DOI：10.1016/j.bmc.2008.09.010

• osteomyelitis
• fluoroquinolone
• bisphosphonates
• drug delivery
• prodrug

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.

• 出版日期2008-10-15