33331-59-8Relevant articles and documents
Synthesis and biological evaluation of the thionated antibacterial agent nalidixic acid and its organoruthenium(II) complex
Hudej, Rosana,Kljun, Jakob,Turk, Boris,Turel, Iztok,Miklavcic, Damijan,Kandioller, Wolfgang,Hartinger, Christian G.,Keppler, Bernhard K.,Repnik, Urska
, p. 5867 - 5874,8 (2012)
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 cytotoxicity 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.
Re-engineering nalidixic acid's chemical scaffold: A step towards the development of novel anti-tubercular and anti-bacterial leads for resistant pathogens
Peraman, Ramalingam,Varma, Raghu Veer,Reddy, Y. Padmanabha
, p. 4314 - 4319 (2015)
Occurrence of antibacterial and antimycobacterial resistance stimulated a thrust to discover new drugs for infectious diseases. Herein we report the work on re-engineering nalidixic acid's chemical scaffold for newer leads. Stepwise clubbing of quinoxaline, 1,2,4-triazole/1,3,4-oxadiazole with nalidixic acid yielded better compounds. Compounds were screened against ciprofloxacin resistant bacteria and Mycobacterium tuberculosis H37Rv species. Results were obtained as minimum inhibitory concentration, it was evident that molecule with quinoxaline linked azide as side chain served as antitubercular lead (6.25 μg/ml) whilst molecule with oxadiazole or triazole linked quinoxaline side chain served as anti-bacterial lead. Few compounds were significantly active against Escherichia coli and Proteus vulgaris with MIC less than 0.06 μg/ml and relatively potent than ciprofloxacin. No true compound was potentially active against Salmonella species as compared to amoxicillin.
Towards calixarene-based prodrugs: Drug release and antibacterial behaviour of a water-soluble nalidixic acid/calix[4]arene ester adduct
Dibama, Hugues Massimba,Clarot, Igor,Fontanay, Stephane,Salem, Adel Ben,Mourer, Maxime,Finance, Chantal,Duval, Raphael E.,Regnouf-de-Vains, Jean-Bernard
scheme or table, p. 2679 - 2682 (2010/02/28)
A water-soluble calixarene-based heterocyclic podand incorporating a quinolone antibiotic subunit, the nalidixic acid, was synthesised and fully characterised. Its prodrug behaviour was assessed in vitro by HPLC, demonstrating the release of the tethered