Synthesis and Biological Evaluation of the Thionated Antibacterial Agent Nalidixic Acid and Its Organoruthenium(II) Complex

Author(s)
Rosana Hudej, Jakob Kljun, Wolfgang Kandioller, Urska Repnik, Boris Turk, Christian G. Hartinger, Bernhard Keppler, Damijan Miklavcic, Iztok Turel
Abstract

The thionated derivative of the antibacterial agent nalidixic acid and its organoruthenium complex were prepared, and their crystal structures were determined. The aqueous stability of the complex was studied and, unlike the case for the nalidixicato complex, increased stability of the ruthenium complex in aqueous solution was observed with only a minor degree of thionalidixicato ligand dissociated within 1 week. While the derivatization caused the antibacterial activity of the ligand against E. coli to decrease, the cytotcodcity of the complex against three cancer cell lines was significantly increased and the inhibitory potency against two enzymes of the cathepsin family was increased by 10-fold.

Organisation(s)
Department of Inorganic Chemistry
External organisation(s)
University of Ljubljana, Jožef Stefan Institute (IJS), University of Auckland
Journal
Organometallics
Volume
31
Pages
5867-5874
No. of pages
8
ISSN
0276-7333
DOI
https://doi.org/10.1021/om300424w
Publication date
2012
Peer reviewed
Yes
Austrian Fields of Science 2012
104003 Inorganic chemistry, 104015 Organic chemistry
Sustainable Development Goals
SDG 3 - Good Health and Well-being
Portal url
https://ucrisportal.univie.ac.at/en/publications/5cc6dfc1-b4c7-4a2b-88aa-f247497b03ef