Literature DB >> 3293524

Comparative in vitro activity of a new fluorinated 4-quinolone, T-3262 (A-60969).

A M Espinoza1, N X Chin, A Novelli, H C Neu.   

Abstract

The in vitro activity of a new quinolone, T-3262 [A-60969; DL-7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1-, 4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid monohydrate], was compared with those of ciprofloxacin, ofloxacin, ceftazidime, imipenem, and gentamicin. T-3262 inhibited 90% of isolates of the family Enterobacteriaceae at a concentration of less than or equal to 0.25 micrograms/ml. It was two to four times more active than ofloxacin and similarly or slightly less active than ciprofloxacin. Ninety percent of isolates of Pseudomonas aeruginosa were inhibited at 0.5 micrograms/ml. It was 4- to 8-fold more active than ciprofloxacin and 8- to 16-fold more active than ofloxacin against Pseudomonas cepacia and Pseudomonas maltophilia, which were resistant to imipenem and gentamicin. Most Haemophilus influenzae, Neisseria gonorrhoeae, and Branhamella catarrhalis isolates were inhibited at concentrations of less than or equal to 0.008 micrograms/ml. The MIC for 90% of the Staphylococcus aureus isolates, including methicillin-resistant S. aureus, was 0.12 micrograms/ml; that for Staphylococcus epidermidis was 0.5 micrograms/ml, as was that for Enterococcus faecalis. It inhibited 90% of Bacteroides fragilis isolates at 2 micrograms/ml, considerably more active than ciprofloxacin and ofloxacin. The frequency of spontaneous point mutational resistance was less than 10(-10) for members of the family Enterobacteriaceae and Pseudomonas spp. Resistant strains could be selected by repeated subculture. Similar to other quinolones, its activity could be affected by culture conditions. T-3262 showed a postantibiotic suppressive effect on Escherichia coli, P. aeruginosa, and S. aureus.

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Year:  1988        PMID: 3293524      PMCID: PMC172249          DOI: 10.1128/AAC.32.5.663

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  7 in total

1.  The fluoroquinolones: structures, mechanisms of action and resistance, and spectra of activity in vitro.

Authors:  J S Wolfson; D C Hooper
Journal:  Antimicrob Agents Chemother       Date:  1985-10       Impact factor: 5.191

2.  In vitro activity of Ro 23-6240, a new fluorinated 4-quinolone.

Authors:  N X Chin; D C Brittain; H C Neu
Journal:  Antimicrob Agents Chemother       Date:  1986-04       Impact factor: 5.191

3.  Differences in susceptibility to quinolones of outer membrane mutants of Salmonella typhimurium and Escherichia coli.

Authors:  K Hirai; H Aoyama; T Irikura; S Iyobe; S Mitsuhashi
Journal:  Antimicrob Agents Chemother       Date:  1986-03       Impact factor: 5.191

4.  Method of reliable determination of minimal lethal antibiotic concentrations.

Authors:  R D Pearson; R T Steigbigel; H T Davis; S W Chapman
Journal:  Antimicrob Agents Chemother       Date:  1980-11       Impact factor: 5.191

5.  The comparative in-vitro activity of eight newer quinolones and nalidixic acid.

Authors:  A King; I Phillips
Journal:  J Antimicrob Chemother       Date:  1986-11       Impact factor: 5.790

6.  Factors influencing the in vitro activity of two new aryl-fluoroquinolone antimicrobial agents, difloxacin (A-56619) and A-56620.

Authors:  L Hirschhorn; H C Neu
Journal:  Antimicrob Agents Chemother       Date:  1986-07       Impact factor: 5.191

7.  Post-antibiotic suppressive effect of ciprofloxacin against gram-positive and gram-negative bacteria.

Authors:  N X Chin; H C Neu
Journal:  Am J Med       Date:  1987-04-27       Impact factor: 4.965

  7 in total
  25 in total

1.  In vitro activity of sparfloxacin.

Authors:  N X Chin; J W Gu; K W Yu; Y X Zhang; H C Neu
Journal:  Antimicrob Agents Chemother       Date:  1991-03       Impact factor: 5.191

2.  In vitro and in vivo antibacterial activities of E-4497, a new 3-amine-3-methyl-azetidinyl tricyclic fluoroquinolone.

Authors:  D Gargallo-Viola; M Esteve; S Llovera; X Roca; J Guinea
Journal:  Antimicrob Agents Chemother       Date:  1991-03       Impact factor: 5.191

3.  In vitro activity of tosufloxacin, a new quinolone, against respiratory pathogens derived from cystic fibrosis sputum.

Authors:  A G Arguedas; J C Akaniro; H R Stutman; M I Marks
Journal:  Antimicrob Agents Chemother       Date:  1990-11       Impact factor: 5.191

4.  Comparative in vitro activity of WIN 57273, a new fluoroquinolone antimicrobial agent.

Authors:  G M Eliopoulos; K Klimm; L B Rice; M J Ferraro; R C Moellering
Journal:  Antimicrob Agents Chemother       Date:  1990-06       Impact factor: 5.191

5.  In vitro and in vivo activities of a new quinolone, WIN 57273, possessing potent activity against gram-positive bacteria.

Authors:  D M Sedlock; R A Dobson; D M Deuel; G Y Lesher; J B Rake
Journal:  Antimicrob Agents Chemother       Date:  1990-04       Impact factor: 5.191

6.  Value of new quinolones in the treatment and prophylaxis of infectious diseases: introductory remarks.

Authors:  J S Wolfson; B E Murray
Journal:  Eur J Clin Microbiol Infect Dis       Date:  1989-12       Impact factor: 3.267

7.  Inhibitory effects of ciprofloxacin and sparfloxacin on DNA gyrase purified from fluoroquinolone-resistant strains of methicillin-resistant Staphylococcus aureus.

Authors:  J Okuda; S Okamoto; M Takahata; T Nishino
Journal:  Antimicrob Agents Chemother       Date:  1991-11       Impact factor: 5.191

8.  In vitro activity of tosufloxacin (A-61827; T-3262) against selected genital pathogens.

Authors:  J Segreti; D J Hirsch; A A Harris; K S Kapell; H Orbach; H A Kessler
Journal:  Antimicrob Agents Chemother       Date:  1990-06       Impact factor: 5.191

9.  WIN 57273, a new fluoroquinolone with enhanced in vitro activity versus gram-positive pathogens.

Authors:  G W Kaatz; S M Seo
Journal:  Antimicrob Agents Chemother       Date:  1990-07       Impact factor: 5.191

10.  Trovafloxacin is active against Toxoplasma gondii.

Authors:  A A Khan; T Slifer; F G Araujo; J S Remington
Journal:  Antimicrob Agents Chemother       Date:  1996-08       Impact factor: 5.191

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