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At least 19 recordsLinked to original sources
PubMed1983

Activity of AT-2266 compared with those of norfloxacin, pipemidic acid, nalidixic acid, and gentamicin against various experimental infections in mice.

AT-2266 (1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1, 8-naphthyridine-3-carboxylic acid) showed marked activity in vivo when administered orally to mice bearing systemic, pulmonary, dermal, or urinary tract infections due to variety of organisms. The activity of AT-2266 was uniformly higher than those of norfloxacin, pipemidic acid, and nalidixic acid against all of the infections. The activity of AT-2266 administered orally was almost comparable to that of gentamicin administered subcutaneously against urinary tract infections due to gram-negative organisms but was generally lower against other infections. AT-2266 exhibited significant activity against infections due to gentamicin-resistant and nalidixic acid-resistant organisms.

Animals↗
PubMed1991

Avian myeloblastosis virus reverse transcriptase inhibition by nalidixic acid.

Nalidixic acid, a very specific inhibitor of bacterial DNA synthesis, has been studied for its action on the avian myeloblastosis virus reverse transcriptase activity. The drug inhibited the DNA synthesis reaction catalyzed by the viral enzyme in the presence of different template-primers. The inhibitory effect by nalidixic acid was higher with polyriboadenylic acid than with polyribocytidylic acid as a synthetic template. With activated DNA as a template nalidixic acid preferentially inhibited the TMP incorporation when compared with the dAMP incorporation. Both these results showed the importance of the presence of adenine in the templates for a more efficient inhibition by nalidixic acid. The inhibition for this drug was also shown in the presence of Mn2+ instead of Mg2+ as the divalent cation, and with a 2'-fluorinated analogue of polyriboadenylic acid as the template. Kinetic data showed a non-competitive inhibition by nalidixic acid in relation to polyriboadenylic acid and to TTP in the reaction catalyzed by reverse transcriptase.

Avian Myeloblastosis Virus↗
PubMed1983

Comparative activities of ciprofloxacin (Bay o 9867), norfloxacin, pipemidic acid, and nalidixic acid.

An agar dilution method was used to measure the minimal inhibitory concentrations of ciprofloxacin (Bay o 9867), norfloxacin, pipemidic acid, and nalidixic acid against 496 clinical isolates. Ciprofloxacin and norfloxacin were active against all species tested (90% minimal inhibitory concentrations less than or equal to 8 micrograms/ml), although ciprofloxacin was somewhat more active, e.g., against gram-positive cocci. Pipemidic acid and nalidixic acid were active against most of the members of the Enterobacteriaceae, but Klebsiella species and Providencia stuartii were only inhibited by a high concentration of nalidixic acid.

Anti-Bacterial Agents↗
PubMed2000

[Color reactions for identification of nalidixic acid].

Nalidixic acid (1) gives with 2-naphthol a yellow charge-transfer complex. The 7-methyl group of 1 condenses with vanillin (2) and Ehrlich's reagent (4) to the coloured (E)-benzylidene compounds 3 and 5. Treating 1 with thionyl chloride and subsequent reaction with aminopyrazolone (6) and sodium acetate leads to a mixture of trichloronalidixic acid (7) and its 3-carboxamide 8. The trichloromethyl group of 7 is converted with 6 in pyridine to form the amide 9. Nalidixic acid reacts with 1,3-dimethylbarbituric acid (10) in acetanhydride/acetic acid to yield the polymethine dyes 11-13, whose structures are confirmed by X-ray crystal structure analysis. The dyes 3 and 12 inhibit the growth of staphylococcus aureus and Escherichia coli, respectively.

Anti-Infective Agents↗
PubMedDate not supplied

Treatment of bacillary dysentery in Vietnamese children: two doses of ofloxacin versus 5-days nalidixic acid.

Nalidixic acid (NA: 55 mg/kg daily for 5 days) is the recommended treatment for uncomplicated bacillary dysentery in areas where multidrug-resistant Shigella are prevalent. An open randomized comparison of this NA regimen with 2 doses of ofloxacin (total 15 mg/kg) was conducted in 1995/96 in 135 Vietnamese children with fever and bloody diarrhoea. Sixty-six children with a bacterial pathogen isolated were eligible for analysis. Of the 63 Shigella isolates, 39 (62%) were resistant to multiple antibiotics. Resolution times for fever and diarrhoea were similar in the 2 groups, but excretion time of stool pathogen was significantly longer in the NA recipients [median (range) days 1 (1-9) vs 1 (1-2), P = 0.001]. There were 9 (25%) treatment failures in the NA regimen and 3 (10%) in the ofloxacin group; P = 0.1. Two patients had NA-resistant Shigella flexneri. One of these isolates was selected during NA treatment. From a clinical and public health standpoint a 2-dose regimen of ofloxacin is preferable to nalidixic acid in the treatment of bacillary dysentery.

Adolescent↗
PubMed1979

[Antibacterial in-vitro activity of pipemidic acid and nalidixic acid (author's transl)].

The in-vitro activity of nalidixic acid and pipemidic acid was investigated in a combined study in 450 freshly isolated bacterial strains using the agar dilution test. Gram-positive cocci were resistant to both substances except for a few pipemidic acid sensitive staphylococci. Both substances had good antibacterial activity in the gram-negative spectrum. However, the MIC values of pipemidic acid were generally clearly lower than those of nalidixic acid. Only pipemidic acid showed activity against Pseudomonas aeruginosa. Thus the in-vitro results showed that pipemidic acid has clear-cut and valuable advantages for the treatment of urinary tract infections when compared with nalidixic acid.

Anti-Bacterial Agents↗
PubMed1991

Nalidixic acid prodrugs: amides from amino acid ester and nalidixic acid.

Amides from amino acid ester and nalidixic acid were synthesized. The solubility characteristics and partition coefficient of the compounds were studied. The hydrolysis of the compounds was studied in the simulated gastric fluid and simulated intestinal fluid. Some compounds showed better antibacterial activity than nalidixic acid.

Amides↗
PubMed1980

Lack of induction of dominant lethal mutations in male mice by nalidixic acid.

Nalidixic acid (NA) in single or in 5 consecutive daily doses of 100 or 1000 mg/kg produced no dominant lethal mutational effects in male ddY strain mice during an 8-week mating schedule. Ethylmethanesulfonate (EMS), used as a positive control, produced dominant lethal mutations in the first and second weeks.

Animals↗
PubMed1998

Site-specific hydroxylation at polyguanosine in double-stranded DNA by UVA radiation with nalidixic acid.

Nalidixic acid (NA) has been used for urinary tract infections and has been reported to be photocarcinogenic. We examined the mechanism of damage to 32P-labeled DNA fragments obtained from the human c-Ha-ras-1 proto-oncogene and the p53 tumor suppressor gene exposed to 365-nm UVA light in the presence of NA. NA plus UVA light caused damage to the double-stranded DNA fragment at consecutive guanine residues, whereas damage to the single-stranded DNA fragment was caused at single guanines and thymines. The formation of 8-oxo-7, 8-dihydro-2'-deoxyguanosine in native DNA exceeded that in denatured DNA at high NA concentrations. The ESR spin destruction method suggested that DNA damage was caused through electron transfer from guanine residues to photoexcited NA. On the basis of these findings, it is concluded that NA can cause skin cancer through DNA damage mediated by its photoactivation.

Base Sequence↗
PubMed1996

Species differences in the disposition and metabolism of nalidixic acid.

Nalidixic acid (NA) is an antimicrobial drug that has been used to treat urinary tract infections. A study of NA by the National Toxicology Program indicated that chronic administration in the diet at doses equivalent to 82 and 175 mg/kg/day for rats, and 175 and 475 mg/kg/day for mice resulted in neoplastic lesions in the preputial and clitoral glands of male and female Fischer 344 rats, respectively, but not in male and female B6C3F1 mice. Our study was designed to evaluate the metabolic basis of this species and tissue-dependent carcinogenicity. [14C]NA was administered by oral gavage as a suspension in corn oil at doses of 20, 200 or 500 mg/kg. Based on urinary excretion data, at least 35 to 46 and 57 to 79% of dose was absorbed from the gastrointestinal tracts of mice and rats, respectively. NA-derived radioactivity was excreted primarily in urine and feces. The urinary and fecal metabolite profiles were species dependent. At 72 hr after administration, in both genders of rats and mice, the highest concentrations of radioactivity were observed in the liver, and the lowest were in the brain and adipose tissue. The preputial and clitoral glands of male and female rats, respectively, contained consistently and substantially higher concentrations of radioactivity compared to all other tissues, with the exception of liver. In mice, the levels of radioactivity in these tissues were near or below quantifiable levels. The metabolism and disposition characteristics of NA were linear in male and female mice over a dose range of 20 to 500 mg/kg: in rats, they were dose dependent. Results of this study suggest that the species- and tissue-dependent differences in carcinogenicity of NA were associated with differences in metabolism and disposition between the two species.

Animals↗
PubMed1978

In vitro activity of oxolinic acid and nalidixic acid against common urinary pathogens: a comparative study.

A study was carried out to compare the sensitivity of 500 bacterial strains, isolated from patients with urinary tract infections, to oxolinic acid and nalidixic acid. The results showed that whilst both antibacterial agents were similar in their bacterial spectrum they were not identical in terms of cross-sensitivity or resistance. Where there was a difference in sensitivity, this was always in flavour of oxolinic acid and was particularly evident in the case of Staphylococcus, Pseudomonas, Serratia, Klebsiella, Proteus (especially P. rettgeri), and to a lesser extent Citrobacter.

Bacteria↗
PubMed1995

Positive R plasmid mutator effect on chromosomal mutation to nalidixic acid resistance in nalidixic acid-exposed cultures of Escherichia coli.

Mutation frequencies to nalidixic acid resistance (15 mg/L in nutrient agar) were determined for derivatives of Escherichia coli AB1157 carrying the mutator plasmids R46, R391 or pYD1, or the non-mutator plasmid RP4. Frequencies of mutation remained constant in cultures of AB1157(R46) growing exponentially in drug-free broth, at a level about 12-fold higher than in the strain without plasmid. Mutation frequencies in cultures of strains AB1157(R391) and AB1157(pYD1) were about three times greater than in the control, whereas plasmid RP4 had no effect on spontaneous mutation frequency to nalidixic acid resistance. Exposure of strain AB1157 to 6 mg/L nalidixic acid in nutrient broth killed 80% of cells after 4 h. This enriched the proportion of nalidixic acid-resistant cells present in the surviving cell population giving enhanced "apparent" mutation frequencies. These were further increased by cell division of resistant mutants in the nalidixic acid-containing medium. "Apparent" resistance mutation frequencies in nalidixic acid-exposed cultures of the R46-, R391- or pYD1-carrying derivatives were, at their peak, 447-, 53- and 38-fold higher than in the control, the strain without plasmid, or the RP4-containing strain, respectively. These data illustrate how mutator plasmids like R391 and pYD1, which mediate only small increases in spontaneous mutation, can contribute to the development of clinically-significant levels of quinolone resistance.

Conjugation, Genetic↗
PubMed1974

Inhibition of ribonucleic acid synthesis by nalidixic acid in Escherichia coli.

The effect of low concentrations of nalidixic acid on ribonucleic acid (RNA) synthesis in Escherichia coli was examined. It was observed that RNA synthesis in exponentially growing cells was not significantly affected, in harmony with previous studies. However, RNA synthesis was markedly depressed by nalidixic acid during starvation for an amino acid or during chloramphenicol treatment. This effect was not caused by increased killing or inhibition of nucleoside triphosphate synthesis by nalidixic acid. The pattern of radioactive uracil incorporation into transfer RNA or ribosomes was not changed by the drug. The sensitivity of RNA synthesis to nalidixic acid in the absence of protein production may be useful in probing the amino acid control of RNA synthesis.

Amino Acids↗