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Infections
Published in Evelyne Jacqz-Aigrain, Imti Choonara, Paediatric Clinical Pharmacology, 2021
Evelyne Jacqz-Aigrain, Imti Choonara
Nalidixic acid is only active against enterobacteria and its use is limited to the treatment of urinary tract infection. Ciprofloxacin has a greater degree of activity than nalidixic acid against Gram-negative rods and is particularly active against P. aeruginosa. Dosage may be adapted according to pharmacokinetics [29]. The newer fluoroquinolone moxifloxacin is also active against Streptococcus pneumoniae.
High-Performance Liquid Chromatography
Published in Adorjan Aszalos, Modern Analysis of Antibiotics, 2020
Joel J. Kirschbaum, Adorjan Aszalos
Nalidixic acid is used intravenously to treat systemic infections, especially those of the urinary tract. To determine nalidixic acid and its active metabolite, hydroxynalidixic acid, in plasma, an octadecylsilane column was used with a mobile phase of water-methanol-cetrimonium bromide (cetrimide) (50:50:0.12) flowing at 1.5 ml/min into a detector set to 313 nm [455]. The limit of detection of 1 μg/ml is well below the therapeutic range of 20—50 μg/ml. Recoveries are approximately 90%. Contents in plasma and urine were assayed using an amino-cyano column and a mobile phase of methanol-0.1 M citrate buffer, pH 3 (95:15 [sic]), flowing at 1.6 ml/min. Detection at 254 nm gave limits of detection of 0.08 μg/ml plasma and 0.42 μg/ml urine [456].
Prospects of Pre-clinical [6.6.0] Bicyclic Nitrogen Heterocycles in the Treatment of Tuberculosis
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Neha P. Agre, Mariam S. Degani, Sanjib Bhakta
Nalidixic acid (61) is known for its outstanding anti-bacterial potential, particularly towards Gram negative organisms, and it contains the 1,8-naphthyridine scaffold which made it worthwhile to explore for its anti-mycobacterial properties.
DFT based QSAR study on quinolone-triazole derivatives as antibacterial agents
Published in Journal of Receptors and Signal Transduction, 2022
Niloofar Ghasedi, Shahin Ahmadi, Sepideh Ketabi, Ali Almasirad
The accidental discovery of Nalidixic acid led to the development of a class of antibacterial drugs called fluoroquinolones. Today, quinolones are among the most important synthetic antibacterial agents, widely used in treating various infections. The clinical success of quinolones is due to features such as good bioavailability in oral administration, good tissue permeability, and relatively low toxicity. However, this widely used antibiotic class has been prone to resistance too. So there is the need to search for new representatives of this class, which have a potent antibacterial activity and the potential to overcome the bacterial resistance [2,3]. Hybrid molecules are chemical structures containing two or more structural domains with different biological functions and dual activities. Such hybrid molecules can overcome cross-drug resistance, create a broader range of effects, reduce toxicity, improve efficacy, and present new candidates with high potency against drug-resistant and drug-sensitive bacteria [1].
Bacterial death from treatment with fluoroquinolones and other lethal stressors
Published in Expert Review of Anti-infective Therapy, 2021
For an ROS scenario to be viable, a source of ROS must be available. It has been known for decades that rapid cessation of further killing by nalidixic acid occurs when a bacteriostatic inhibitor of protein synthesis (chloramphenicol) is added to cultures of E. coli [36] (a sub-inhibitory combination of thiourea and bipyridyl has the same effect as chloramphenicol (X. Wang, X. Zhao, and K. Drlica, unpublished observations)). The principle also applies to norfloxacin and ampicillin when a variety of bacteriostatic agents are subsequently added [34]. The phenomenon is explained by bacteriostatic agents blocking the elevated respiration needed to maintain elevated ROS levels [34]. Exactly how antibiotic treatment triggers excessive ROS production remains to be discovered. We speculate that antimicrobial stress either transiently over-activates the respiratory chain or slows the electron transfer from the ‘reduced state’ flavin-containing respiratory enzymes, either of which could elevate ROS production.
Opioid use potentiates the virulence of hospital-acquired infection, increases systemic bacterial dissemination and exacerbates gut dysbiosis in a murine model of Citrobacter rodentium infection
Published in Gut Microbes, 2020
Fuyuan Wang, Jingjing Meng, Li Zhang, Sabita Roy
The C. rodentium strain (DBS 100) was obtained from American Type Culture Collection (ATCC; Manassas, VA). Nalidixic acid resistant C. rodentium was selectively screened on LB agar plates with 20 μg/ml nalidixic acid. A spontaneous mutant of C. rodentium DBS100 that was resistant to nalidixic acid (20 μg/ml) was obtained by growing DBS100 at 37°C in LB medium supplemented with nalidixic acid at 5 μg/ml for 7 h before spreading the liquid culture onto LB agar plates that were supplemented with nalidixic acid at 20 μg/ml. The selective LB agar plates and broth were made by adding up to 20 μg/ml nalidixic acid to selectively culture C. rodentium in the future study.52 The nalidixic acid solution was made with Mili-Q water in fume hood, and the stock solution was sterilized through a 0.22 μm filter using a 10-ml syringe in the sterile hood. Kanamycin-resistant C. rodentium was obtained from the laboratory of Dr. Bruce A. Vallance at the University of British Columbia, Vancouver, Canada.53 Bioluminescent strains of C. rodentium were constructed by introducing the plasmid pT7, which carried the entire lux operon from Photorhabdus luminescens. For selective culture of C. rodentium, kanamycin (SKU 60615, Sigma) was added into the Luria-Bertani broth or agar plates at a concentration of 30 μg/ml.