title: Synthesis of osteotropic hydroxybisphosphonate derivatives of fluoroquinolone antibacterials.
abstract: 1-Hydroxybisphosphonate derivatives of ciprofloxacin, gatifloxacin and moxifloxacin have been synthesized using Cu(I) catalyzed azide-alkyne 1,3-dipolar cycloaddition reaction. The 1,2,3-triazol linked hydroxybisphosphonate derivative of ciprofloxacin exhibited antibacterial activity comparable to the parent antibiotic and all fluoroquinolone-bisphosphonates displayed osteotropic properties in a bone model.
authors.affiliation: Department of Clinical Investigation, Eisenhower Army Medical Center, Fort Gordon, GA, USA.
authors.forename: James C
authors.initials: JC
authors.lastname: McPherson
authors.forename: Royce
authors.initials: R
authors.lastname: Runner
authors.forename: Thomas B
authors.initials: TB
authors.lastname: Buxton
authors.forename: John F
authors.initials: JF
authors.lastname: Hartmann
authors.forename: Dan
authors.initials: D
authors.lastname: Farcasiu
authors.forename: Ilona
authors.initials: I
authors.lastname: Bereczki
authors.forename: Erzsébet
authors.initials: E
authors.lastname: Roth
authors.forename: Szilvia
authors.initials: S
authors.lastname: Tollas
authors.forename: Eszter
authors.initials: E
authors.lastname: Ostorházi
authors.forename: Ferenc
authors.initials: F
authors.lastname: Rozgonyi
authors.forename: Pál
authors.initials: P
authors.lastname: Herczegh
mesh_terms: D000327:Adsorption; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001842:Bone and Bones / Q000187:drug effects / Q000378:metabolism; D017886:Durapatite / Q000737:chemistry / Q000378:metabolism; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D049329:Nanostructures; D063065:Organophosphonates / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D063065:Organophosphonates; D017886:Durapatite