Quinolone antibacterial agents linked to osteotropic bisphosphonate moieties

Author(s)
Thomas Pieper, Bernhard Keppler
Abstract

Bisphosphonates are widely used in diagnosis and therapy of different bone diseases. Due to their potential to accumulate in the inorganic bone matrix hydroxylapatite they are useful agents in osteotic vectorization of different types of drugs. We linked bisphosphonate moieties to antibacterial quinolones like norfloxacin to enable a selective targeting of these agents to bone tissue. The quinolones (1,4-dihydro-4-oxo-quinoline-3-carboxylic acids) were modified at position 1 and 7 using alkylbisphosphonates with ethene-, amino- and carboxylic-groups. After coupling with the quinolones, the alkylbisphosphonic esters could smoothly be hydrolyzed via the corresponding silyl esters to obtain the free bisphosphonic acids.

Organisation(s)
Department of Inorganic Chemistry
External organisation(s)
University of Vienna
Journal
Phosphorus, Sulfur and Silicon and the Related Elements
Volume
170
Pages
5-14
No. of pages
10
ISSN
1042-6507
DOI
https://doi.org/10.1080/10426500108040581
Publication date
2001
Peer reviewed
Yes
Austrian Fields of Science 2012
1040 Chemistry
Portal url
https://ucrisportal.univie.ac.at/en/publications/bf27f2a6-fb83-40ad-b7fa-9c62744d2187