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Synthesis of osteotropic hydroxybisphosphonate derivatives of fluoroquinolone antibacterials
James C McPherson1, Royce Runner, Thomas B Buxton
1Department of Clinical Investigation, Eisenhower Army Medical Center, Fort Gordon, GA, USA.
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.
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