| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1396000 | European Journal of Medicinal Chemistry | 2012 | 4 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Bisphosphonate derivatives of antibiotics are osteotropic compounds. ► New hydroxibisphosphonate derivatives of fluoroquinolone antibacterials were synthesized. ► The fluoroquinolone-bisphosphonate conjugates strongly adsorb on hydroxyapatite bone model. ► The conjugates have antibacterial activity. ► The new compounds will be evaluated for treatment of osteomyelitis.
