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International Urology and Nephrology 1976The absorption, distribution and excretion of piromidic acid and its ethyl ester were investigated in the rat. When administered orally the ethyl ester was well absorbed... (Comparative Study)
Comparative Study
The absorption, distribution and excretion of piromidic acid and its ethyl ester were investigated in the rat. When administered orally the ethyl ester was well absorbed and subsequently hydrolysed, giving much higher blood and tissue concentration than a corresponding dose of the parent compound. The antimicrobial activity of urine and bile samples was also investigated.
Topics: Animals; Chemical Phenomena; Chemistry; Intestinal Absorption; Nicotinic Acids; Pyrrolidines; Rats
PubMed: 965200
DOI: 10.1007/BF02081992 -
Chemical & Pharmaceutical Bulletin Jul 1976
Topics: Animals; Anti-Infective Agents; Kinetics; Male; Rats
PubMed: 975418
DOI: 10.1248/cpb.24.1462 -
Square wave adsorptive stripping voltammetric determination of piromidic acid. Application in urine.Journal of Pharmaceutical and... Nov 2003A simple procedure for the determination of piromidic acid by square wave adsorptive stripping voltammetry (SW-AdSV) at a hanging mercury drop electrode has been...
A simple procedure for the determination of piromidic acid by square wave adsorptive stripping voltammetry (SW-AdSV) at a hanging mercury drop electrode has been developed. The variables affecting to accumulation process such as concentration of perchloric acid, accumulation potential and accumulation time have been optimised (0.025 mol L(-1), -0.25 V and 140 s, respectively) by using response surface methodology. A linear relationship between concentration of piromidic acid and peak intensity has been found in the range 2.22 x 10(-9) to 3.33 x 10(-8) mol L(-1). The detection limit (1.65 x 10(-9) mol L(-1)) has been calculated by the method proposed by Clayton et al. so that protection against both false positive and false negative errors is assured. The procedure was successfully applied to determine piromidic acid in spiked urine samples. The obtained recovery values were in the range 97.3-103.3% at different levels of concentration of piromidic acid.
Topics: Electrochemistry; Piromidic Acid
PubMed: 14623580
DOI: 10.1016/s0731-7085(03)00306-6 -
Chemical & Pharmaceutical Bulletin Jul 1976
Topics: Animals; Anti-Infective Agents; Bile; Humans; Male; Nicotinic Acids; Pyrrolidines; Rats
PubMed: 975416
DOI: 10.1248/cpb.24.1433 -
Antimicrobial Agents and Chemotherapy Aug 1975Pipemidic acid, 8-ethyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)-pyrido [2,3-d]pyrimidine-6-carboxylic acid, is a new derivative of piromidic acid. It is active against...
Pipemidic acid, 8-ethyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)-pyrido [2,3-d]pyrimidine-6-carboxylic acid, is a new derivative of piromidic acid. It is active against gram-negative bacteria including Pseudomonas aeruginosa as well as some gram-positive bacteria. Its potency is generally greater than that of piromidic acid and nalidixic acid. Cross-resistance is not observed between pipemidic acid and various antibiotics, and most of bacteria resistant to piromidic acid and nalidixic acid are moderately susceptible to pipemidic acid. The activity of pipemidic acid is scarcely affected by the addition of serum, sodium cholate, or change of medium pH, but is subject to the influence of inoculum size. Its action is bactericidal above minimal inhibitory concentrations.
Topics: Bacteria; Drug Resistance, Microbial; Microbial Sensitivity Tests; Nicotinic Acids; Piperazines; Pseudomonas aeruginosa
PubMed: 810076
DOI: 10.1128/AAC.8.2.132 -
Il Farmaco; Edizione Scientifica Feb 1984The synthesis and antibacterial activities of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid are reported. The new analog of nalidixic acid has...
Researches on antibacterial and antifungal agents. II - Synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid, a novel highly active, broad-spectrum antibacterial agent related to piromidic acid.
The synthesis and antibacterial activities of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid are reported. The new analog of nalidixic acid has been prepared by standard procedure starting from 1-(3-aminophenyl)pyrrole; it showed a broad spectrum of antibacterial activity and exhibited much higher activity than nalidixic, pipemidic and piromidic acids. The synthesis of 1-ethyl-1,4-dihydro-4-oxo-8-(1-pyrrolyl)quinoline-3-carboxylic acid is also described; this acid was inactive when tested as antibacterial agent.
Topics: Anti-Bacterial Agents; Anti-Infective Agents; Antifungal Agents; Blastomyces; Candida albicans; Chemical Phenomena; Chemistry; Enterobacteriaceae; Gram-Positive Bacteria; Microbial Sensitivity Tests; Nicotinic Acids; Piromidic Acid; Proteus; Pseudomonas aeruginosa; Pyrrolidines
PubMed: 6425079
DOI: No ID Found -
Chemical & Pharmaceutical Bulletin Sep 1977
Topics: Anti-Infective Agents; Humans; Kinetics; Nicotinic Acids; Pyrrolidines
PubMed: 589722
DOI: 10.1248/cpb.25.2203 -
Antimicrobial Agents and Chemotherapy Aug 1978Spontaneous mutants with various patterns of resistance to pipemidic acid (PPA), piromidic acid (PA), and nalidixic acid (NAL) were isolated from Escherichia coli K-12....
Spontaneous mutants with various patterns of resistance to pipemidic acid (PPA), piromidic acid (PA), and nalidixic acid (NAL) were isolated from Escherichia coli K-12. Most mutants were less resistant to PPA than to PA and NAL, and some mutants resistant to PA and NAL were hypersusceptible to PPA. As for the mutants tested, resistance to the drugs was conferred by mutations at nalA and new nal genes designated as nalC and nalD, both of which were located at about 82 min on the recalibrated map. Resistance to PA and NAL was due to decreased sensitivity of the bacterial DNA synthesizing system to them and insufficient drug transport, whereas resistance to PPA was only due to the former.
Topics: Chromosome Mapping; Conjugation, Genetic; DNA, Bacterial; Drug Resistance, Microbial; Escherichia coli; Mutation; Nalidixic Acid; Nicotinic Acids; Pipemidic Acid; Piromidic Acid; Transduction, Genetic
PubMed: 358918
DOI: 10.1128/AAC.14.2.240 -
The Journal of Applied Bacteriology Apr 1978
Comparative Study
Topics: Anti-Infective Agents, Urinary; Cystitis; Drug Resistance, Microbial; Escherichia coli; Nalidixic Acid; Nicotinic Acids; Piperazines; Pyrrolidines
PubMed: 346547
DOI: 10.1111/j.1365-2672.1978.tb00790.x -
Antimicrobial Agents and Chemotherapy Apr 1976Pipemidic acid, a structural relative of piromidic and nalidixic acids, exhibited substantial therapeutic activity when it was administered orally to mice bearing either... (Comparative Study)
Comparative Study
Pipemidic acid, a structural relative of piromidic and nalidixic acids, exhibited substantial therapeutic activity when it was administered orally to mice bearing either widely disseminated or relatively localized infections with Staphylococcus aureus and a variety of gram-negative bacilli. The activity of pipemidic acid was always greater than that of piromidic and nalidixic acids; in infections with Pseudomonas aeruginosa and in bacilli resistant to the latter two drugs, pipemidic acid exhibited significant activity. In limited comparative studies, the activities of pipemidic acid were generally superior to the activities of cephalexin, ampicillin, and carbenicillin. Gentamicin, administered subcutaneously, was more active than pipemidic acid, given either orally or subcutaneously, against both systemic and localized infections with P. aeruginosa. The therapeutic accomplishments of pipemidic acid were attained with well-tolerated doses.
Topics: Ampicillin; Animals; Anti-Infective Agents; Bacterial Infections; Carbenicillin; Cephalexin; Female; Gentamicins; Kidney Diseases; Lung Diseases; Mice; Nalidixic Acid; Nicotinic Acids; Piperazines; Skin Diseases, Infectious; Urinary Bladder Diseases; Urinary Tract Infections
PubMed: 1267435
DOI: 10.1128/AAC.9.4.569