-
Cancer Letters Jan 1982The formation of nitroso compounds and mutagens from 5 nitrogen-containing drugs (cinnarizine, ethambutol, piromidic acid, pyridinol carbamate and tiaramide) by...
The formation of nitroso compounds and mutagens from 5 nitrogen-containing drugs (cinnarizine, ethambutol, piromidic acid, pyridinol carbamate and tiaramide) by drug/nitrite interaction was examined. On the reaction of 50 micrometers drug and 500 micrometers nitrite at pH 3.0--3.4 and 37 degrees C for 4 h, the considerable formation of nitroso compounds was observed for ethambutol, cinnarizine and pyridinol carbamate. The reaction product of pyridinol carbamate and nitrite was remarkably mutagenic to Salmonella typhimurium TA100 in the absence of S-9 mix. Under conditions presumed to resemble those in the stomach after ingestion of a therapeutic dose of the drug, the formation of nitroso compounds was observed for ethambutol and significant mutagenicity was detected in the reaction product of pyridinol carbamate.
Topics: Benzothiazoles; Cinnarizine; Ethambutol; Mutagens; Nitrites; Nitroso Compounds; Piperazines; Piromidic Acid; Pyridinolcarbamate; Salmonella typhimurium; Thiazoles
PubMed: 7037170
DOI: 10.1016/0304-3835(82)90075-1 -
Journal of Bacteriology Nov 1981In Escherichia coli K-12 mutants which had a new nalidixic acid resistance mutation at about 82 min on the chromosome map, cell growth was resistant to or...
In Escherichia coli K-12 mutants which had a new nalidixic acid resistance mutation at about 82 min on the chromosome map, cell growth was resistant to or hypersusceptible to nalidixic acid, oxolinic acid, piromidic acid, pipemidic acid, and novobiocin. Deoxyribonucleic acid gyrase activity as tested by supercoiling of lambda phage deoxyribonucleic acid inside the mutants was similarly resistant or hypersusceptible to the compounds. The drug concentrations required for gyrase inhibition were much higher than those for cell growth inhibition but similar to those for inhibition of lambda phage multiplication. Transduction analysis with lambda phages carrying the chromosomal fragment of the tnaA-gyrB region suggested that one of the mutations, nal-31, was located on the gyrB gene.
Topics: Bacteriophage lambda; DNA Topoisomerases, Type II; Drug Resistance, Microbial; Escherichia coli; Genes, Bacterial; Mutation; Nalidixic Acid; Transduction, Genetic
PubMed: 6271730
DOI: 10.1128/jb.148.2.450-458.1981 -
The Journal of Antimicrobial... May 1978
Topics: Anti-Bacterial Agents; Dioxolanes; Enterobacteriaceae; Microbial Sensitivity Tests; Nalidixic Acid; Nicotinic Acids; Oxolinic Acid; Staphylococcus aureus
PubMed: 670126
DOI: 10.1093/jac/4.3.289 -
Journal of Chromatography. B,... Oct 1998A rapid high-performance liquid chromatographic method has been developed to determine piromidic acid in trout muscle tissue and in urine, in the presence of nalidixic,...
A rapid high-performance liquid chromatographic method has been developed to determine piromidic acid in trout muscle tissue and in urine, in the presence of nalidixic, 7-hydroxymethylnalidixic, oxolinic and pipemidic acids and cinoxacin. A Nova-Pak C18 column was used with acetonitrile-4x10(-4) M oxalic acid (40:60, v/v) as the mobile phase. A post-column change of pH was made with NaOH. Fluorimetric detection at 456 nm (lambda ex 275 nm) was used. The instrumental detection limit was 5.91 ng/ml, based on height of peak. Pretreatment of the urine samples was not necessary and fish samples were extracted with sodium hydroxide solutions and cleaned by means of an extraction with chloroform. Detection limit was 147 ng/ml for urine and 5.91 ng/g for trout muscle. Good separation without interference from any other components was obtained. Recovery was better than 87% in urine and better than 72% in trout muscle tissue.
Topics: Adult; Animals; Anti-Infective Agents; Chromatography, High Pressure Liquid; Fluorometry; Humans; Hydrogen-Ion Concentration; Muscles; Piromidic Acid; Trout
PubMed: 9832370
DOI: 10.1016/s0378-4347(98)00332-6 -
The Journal of Antimicrobial... Jun 1982
Topics: Enterobacteriaceae; Microbial Sensitivity Tests; Nalidixic Acid; Nicotinic Acids; Piromidic Acid; Staphylococcus aureus
PubMed: 7107550
DOI: 10.1093/jac/9.6.493 -
The Journal of Toxicological Sciences Nov 1978Pipemidic acid (PPA) orally given in a dose of 100 mg/kg/day or more was found to cause lame gait in immature beagle dogs of about 3 months old. Their diarthrodial...
Pipemidic acid (PPA) orally given in a dose of 100 mg/kg/day or more was found to cause lame gait in immature beagle dogs of about 3 months old. Their diarthrodial joints were abnormal with increased synovial fluid and blister formation under the outer layer of the articular cartilage. However, such an abnormality was not found in dogs younger than 2 weeks or older than 12 months. The blisters were formed at the joint areas bearing the body weight at a time when PPA was considered to be present there. Nalidixic and piromidic acids, structural analogues of PPA, also caused abnormality similar to PPA. The severity of the arthropathy was slight with piromidic acid as compared with PPA and nalidixic acid. The gait abnormality was almost disappeared spontaneously even if medication was continued. The incidence of the arthropathy was not or rarely observed in any young rats, rabbits and monkeys.
Topics: Aging; Animals; Dogs; Female; Gait; Haplorhini; Joint Diseases; Macaca; Macaca mulatta; Male; Nalidixic Acid; Nicotinic Acids; Physical Exertion; Pipemidic Acid; Piromidic Acid; Rabbits; Rats; Species Specificity
PubMed: 105148
DOI: 10.2131/jts.3.357 -
Chemical & Pharmaceutical Bulletin Aug 1980
Topics: Bacteria; Nicotinic Acids; Piromidic Acid
PubMed: 7428132
DOI: 10.1248/cpb.28.2531 -
FEMS Microbiology Ecology Feb 2006Inferences about which microorganisms degrade polycyclic aromatic hydrocarbons in contaminated soils have largely been obtained using culture-based techniques, despite...
Inferences about which microorganisms degrade polycyclic aromatic hydrocarbons in contaminated soils have largely been obtained using culture-based techniques, despite the low percentage of microorganisms in soil that are believed to be culturable. We used a substrate-responsive direct viable count method to identify and quantify potential polycyclic aromatic hydrocarbon-degrading bacteria in a soil containing petroleum wastes. Bacteria were extracted and their response to substrates determined in the presence of DNA gyrase inhibitors, which cause viable and active cells to elongate. When yeast extract, a widely used carbon source, was added as a growth substrate, together with nalidixic acid, piromidic acid and ciprofloxacin, a significant increase in elongated cells to 47%, 37% and 22%, respectively, was observed within 24 h. With pyrene as the main substrate, 10 mg L(-1) of nalidixic acid or piromidic acid caused 18-22% and 8-12%, respectively, of the cells to elongate within 24 h; whereas the effect of 0.5 mg L(-1) ciprofloxacin was not significant until 53 h later. Enlarged cells were identified and enumerated by fluorescent in situ hybridization, using Alpha-, Beta- and Gammaproteobacteria, and domain Bacteria-specific probes. The Bacteria-specific probe detected 35-71% of the total microorganisms detected by the DNA-binding dye 4,6-diamidino-2-phenylindole. Initially, 44%, 13% and 5% of the total bacteria in the soil extract were Alpha-, Beta- and Gammaproteobacteria, respectively. Without pyrene or a gyrase inhibitor, these subgroups decreased to 30% of the total population but were predominant with piromidic acid or unchanged with ciprofloxacin when pyrene was the main substrate. The proportion of elongated Alpha- and Betaproteobacteria (potential pyrene degraders) increased significantly (P<0.05). This approach links phylogenetic information with physiological function in situ without the conventional cultivation of bacteria and can be used to probe and enumerate degradative groups at even a finer level of discrimination.
Topics: Anti-Bacterial Agents; Bacteria; Biodegradation, Environmental; Ciprofloxacin; Colony Count, Microbial; Culture Media; DNA, Bacterial; In Situ Hybridization, Fluorescence; Indoles; Nalidixic Acid; Piromidic Acid; Pyrenes; Soil Microbiology; Staining and Labeling
PubMed: 16420636
DOI: 10.1111/j.1574-6941.2005.00035.x -
Annales de Recherches Veterinaires.... 1990Nalidixic acid and similar antimicrobial agents have been available for more than 20 years, mainly for treating infections caused by Gram-negative enterobacteria.... (Review)
Review
Nalidixic acid and similar antimicrobial agents have been available for more than 20 years, mainly for treating infections caused by Gram-negative enterobacteria. Recently, several chemically related drugs, including oxolinic acid, pipemidic acid, piromidic acid and flumequine, have been developed. They are either naphthyridine-carboxylic acid or quinoline-carboxylic acid derivatives and, with nalidixic acid, are so-called quinolones. A major advance in antimicrobial chemotherapy was the synthesis of newer quinolones containing at least 1 fluorine atom and a piperazinyl group. These new fluoroquinolones have an extended antimicrobial spectrum compared to the first quinolone generation, and are highly active against most Gram-negative pathogens including the Enterobacteriaceae and Pseudomonas aeruginosa. The pharmacokinetic properties and residue levels of these quinolones and fluoroquinolones for which clinical experience or experimental information exists in poultry are reviewed here. On the other hand, administration of the quinoxaline-di-N-oxide, olaquindox, for medical purposes raises questions concerning the pharmacokinetic disposition of the drug and the risk of its residues in poultry. This paper presents information about the pharmacokinetic profile of olaquindox and the presence of its residues in chickens.
Topics: 4-Quinolones; Animals; Anti-Infective Agents; Chickens; Drug Residues; Humans; Molecular Structure; Quinoxalines; Tissue Distribution
PubMed: 2080842
DOI: No ID Found -
The Journal of Antimicrobial... Dec 1986Twelve 4-quinolones (cinoxacin, ciprofloxacin, enoxacin, flumequin, nalidixic acid, norfloxacin, oxolinic acid, pefloxacin, pipemidic acid, rosoxacin, and piromidic and...
Twelve 4-quinolones (cinoxacin, ciprofloxacin, enoxacin, flumequin, nalidixic acid, norfloxacin, oxolinic acid, pefloxacin, pipemidic acid, rosoxacin, and piromidic and beta-hydroxypiromidic acids) and novobiocin, were used at subinhibitory concentrations to eliminate from Escherichia coli 11 antibiotic resistance plasmids belonging to different incompatibility groups. The 12 4-quinolones were also tested for their ability to cure virulence plasmids from five species of Enterobacteriaceae. All quinolones eliminated three antibiotic resistance plasmids (R446b, R386, S-a) and one virulence plasmid (pWR105), but at a low rate. Optimal curing of antibiotic resistance plasmids was obtained in human urine. Two virulence plasmids (pWR24 and pWR110) were eliminated only by flumequin and pefloxacin. Novobiocin eliminated three antibiotic resistance plasmids (R446b, R386, pIP24). The variable and low level of plasmid loss may be explained by the induction of the recA system. In addition, the inability to eliminate certain plasmids could be due to their presence in high numbers per cell.
Topics: Culture Media; DNA Transposable Elements; Drug Resistance, Microbial; Enterobacteriaceae; Novobiocin; Plasmids; Quinolines
PubMed: 3029010
DOI: 10.1093/jac/18.6.667