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.

journal_name

Eur J Med Chem

authors

McPherson JC 3rd,Runner R,Buxton TB,Hartmann JF,Farcasiu D,Bereczki I,Roth E,Tollas S,Ostorházi E,Rozgonyi F,Herczegh P

doi

10.1016/j.ejmech.2011.10.049

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

615-8

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00791-4

journal_volume

47

pub_type

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