1985
DOI: 10.1128/aac.27.1.4
|View full text |Cite
|
Sign up to set email alerts
|

In vitro and in vivo antibacterial activities of the fluoroquinolone WIN 49375 (amifloxacin)

Abstract: WIN 49375 (amifloxacin) is a synthetic antibacterial agent of the quinolone class. It is similar in chemical structure to pefloxacin but differs by containing a methylamino, rather than an ethyl, substituent at the 1-N position. The activity of WIN 49375 in vitro was comparable to those of norfloxacin and pefloxacin against Enterobacteriaceae and generally greater than those of tobramycin and cefotaxime. WIN 49375 was more active in vitro than carbenicillin and mezlocillin against Pseudomonas aeruginosa isolat… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1

Citation Types

1
8
0

Year Published

1986
1986
2000
2000

Publication Types

Select...
6
2

Relationship

0
8

Authors

Journals

citations
Cited by 30 publications
(9 citation statements)
references
References 15 publications
1
8
0
Order By: Relevance
“…The piperazinyl N-oxide form of amifloxacin is the major metabolite in rats, while the piperazinyl N-desmethyl form occurs as the primary metabolite in monkeys. The contribution of these metabolites for effective therapeutic use has to await data on human metabolism, but in the animal models the N-oxide metabolite was less efficacious than the parent or N-desmethyl compounds (2,15). This study reflects these findings in that the piperazinyl N-desmethyl form but not the N-oxide form was almost as active in vitro as the parent amifloxacin compound for certain gram-negative bacteria.…”
supporting
confidence: 70%
“…The piperazinyl N-oxide form of amifloxacin is the major metabolite in rats, while the piperazinyl N-desmethyl form occurs as the primary metabolite in monkeys. The contribution of these metabolites for effective therapeutic use has to await data on human metabolism, but in the animal models the N-oxide metabolite was less efficacious than the parent or N-desmethyl compounds (2,15). This study reflects these findings in that the piperazinyl N-desmethyl form but not the N-oxide form was almost as active in vitro as the parent amifloxacin compound for certain gram-negative bacteria.…”
supporting
confidence: 70%
“…On the other hand, the frequency of spontaneous mutants resistant to amifloxacin was about 10-8/CFU. Amifloxacin is a fluoroquinolone and has a broad spectrum and potent activities that are almost comparable to those of norfloxacin and ofloxacin (1,4,(14)(15)(16).…”
Section: Resultsmentioning
confidence: 99%
“…With the exception of anaerobic bacteria (5), MICs of the fluoroquinolones for bacteria tend to be affected little by inoculum size, type of medium, or presence of serum (10,12,54,58). Certain of the compounds, however, exhibit substantially less activity (to 100-fold) in the presence of urine and moderately less activity when the pH of the medium is less than 5 (9, 10, 12, 54, 60).…”
Section: Spectrum Of Antimicrobial Activity In Vitromentioning
confidence: 99%
“…The quinolones characteristically kill bacteria rapidly, with as much as a thousandfold decrease in viability in 1 to 2 h of drug exposure at 1 to 4 times the MIC (9,10,12,14,17,32,53,54). The exact mechahism of killing is not known (14,49), but it might involve cleavage of bacterial chromosomal DNA by DNA gyrase.…”
Section: Mechanisms Of Action and Bacterial Resistancementioning
confidence: 99%
See 1 more Smart Citation