Activities of new quinoline derivatives against genital pathogens

The in vitro activities of three newly developed quinolone drugs and fleroxacin ) against 10 strains of clinically isolated Chiamydia trachomatis were assessed and compared with those of other quinolones and minocycline. T-3262 (MIC for 90% of isolates tested, 0.1 ,ug/ml) was the most active of the quinolones. The NY-198 and fleroxacin MICs for 90% of isolates were 3.13 and 62.5 ,ug/ml, respectively.

supporting

confidence: 76%

mentioning

confidence: 99%

In vitro activities of T-3262, NY-198, fleroxacin (AM-833; RO 23-6240), and other new quinolone agents against clinically isolated Chlamydia trachomatis strains

Maeda

Fujii

Nakata

et al. 1988

“…A-56619 was the most active quinolone against both the lymphogranuloma venereum and occulogenital strains of C. trachomatis tested, having MICs eightfold lower than those of ciprofloxacin. The isolates were fully resistant to norfloxacin, as previously reported (1,9,10,14,17). The agents showed poor activity against G. vaginalis and U. urealyticum.…”

mentioning

confidence: 59%

“…We found most U. urealyticum strains tested to be resistant to the quinolones. Although lower MICs of ciprofloxacin against U. urealyticum have been reported (14), similar MIC ranges have also been documented (1,8,17).…”

mentioning

confidence: 92%

In vitro activity of A-56619 (difloxacin), A-56620, and other new quinolone antimicrobial agents against genital pathogens

Liebowitz¹,

Saunders²,

Fehler³

et al. 1986

The in vitro activities of two new carboxyquinolones, A-56619 (difloxacin) and A-56620, were compared with those of ciprofloxacin, norfloxacin, and ofloxacin against genital tract pathogens. All the quinolones were highly active against Neisseria gonorrhoeae. A-56619 had the lowest MICs against Chlamydia trachomatis (MIC range, 0.125 to 0.25 ,ug/ml) and Haemophilus ducreyi (MIC for 90% of isolates tested, 0.1 ,ug/ml).The newer quinolone antimicrobial agents have been shown to have excellent activity in vitro against gonococci, including ,B-lactamase-producing strains (3,11,13,16,18), and moderate activity in vitro against Chlamydia trachomatis (2,10,14).We compared the activities of A-56619 (difloxacin), A-56620, ciprofloxacin, norfloxacin, ofloxacin, and antimicrobial agents now used for the treatment of genital infections against clinical isolates of Neisseria gonorrhoeae, Haemophilus ducreyi, Gardnerella vaginalis, Ureaplasma urealyticum, and C. trachomatis.Antimicrobial reference standards and sources were as follows: A-56619, A-56620, and erythromycin, Abbott Lab of M. hominis and 2-day-old broth cultures of U. urealyticum were inoculated into 100 ,ul of twice the required final concentration of each of the antibiotic dilutions in U-well microtiter plates. Controls containing medium only, medium plus antimicrobial agent, and medium plus M. hominis or U. urealyticum were included. The microtiter plates were sealed and incubated at 37°C until the indicator in the Mycoplasma-Ureaplasma control well changed color. The MIC was defined as the lowest concentration of antimicrobial agent which prevented color change.MIC testing of C. trachomatis was performed by a modification of a previously described method (15). Inocula of a 1-ml suspension of C. trachomatis in Eagle minimum essential medium supplemented with fetal bovine serum (10% vol/vol), glutamine (1% [vol/vol] of stock solution of 30 mg/ml), and vitamins (1% vol/vol), containing approximately 1.6 x 108 inclusion-forming units per ml, were added to flat-bottomed plastic tubes containing a cover slip monolayer of cycloheximide-treated McCoy cells. After centrifugation at 3,500 x g at 35°C for 60 min, the medium was replaced with 1 ml of supplemental Eagle medium containing the antimicrobial agents tested. The tubes were incubated at 35°C for 48 h. The cover slips were removed, fixed with methanol, stained with iodine, and examined by bright-field illumination for the presence of inclusions. The MIC was defined as the lowest concentration of antimicrobial agent which prevented the appearance of any inclusion bodies.The MICs of the antimicrobial agents tested against isolates of N. gonorrhoeae, H. ducreyi, U. urealyticum, G. vaginalis, and C. trachomatis are shown in Tables 1 and 2. The quinolones, cefotaxime, and ceftazidime were highly active against gonococci, including P-lactamase-producing isolates. A-56619 and A-56620 were the most active quinolones against H. ducreyi. A-56619 was the most active quinolone against both the lymphogranuloma venereum and o...

“…hominis may be inhibited by theoretically attainable concentrations of ciprofloxacin according to a number of studies (14,17,19,26,27,39,46). MICs for other quinolones have also been reported (17,19,20,26,27,33,39,41,46 (1,2,7,15,17,19,26,27,33,39,46).…”

Section: Discussionmentioning

confidence: 99%

In vitro susceptibilities of Mycoplasma pneumoniae, Mycoplasma hominis, and Ureaplasma urealyticum to sparfloxacin and PD 127391

Waites

Duffy

Schmid

et al. 1991

The in vitro activities of two investigational quinolones, sparfloxacin (previously designated AT 4140) and PD 127391, were determined for 30 strains each of Mycoplasma pneumoniae, Mycoplasma hominis, and Ureaplasma urealyticum and compared with those of ciprofloxacin, tetracycline, clindamycin, and erythromycin. Erythromycin was the most active compound against M. pneumoniae (maximum MIC, <0.008 ,ug/ml). PD 127391 (MICs, <0.008 to 0.031 ,ug/ml), sparfloxacin (MICs, <0.008 to 0.25 pg/ml), clindamycin (MICs, <0.008 to 0.5 ,g/ml), and tetracycline (MICs, 0.063 to 0.25 pg/ml) were superior to ciprofloxacin (MICs, 0.5 to 2 ,ug/ml). Sparfloxacin and PD 127391 were active against M. hominis (MICs, <0.008 to 0.031 pg/ml for each) at concentrations comparable to those of clindamycin (MICs, <0.008 to 0.063 ,g/ml) and at concentrations lower than those of ciprofloxacin (MICs, 0.125 to 0.5 pg/ml). As expected, M. hominis was resistant to erythromycin (MICs, 32 to .256 ,ug/ml). For U. urealyticum, PD 127391 (MICs, 0.031 to 0.5 ,ug/ml) and sparfloxacin (MICs, 0.063 to 1 ,ug/ml) were superior to erythromycin (MICs, 0.25 to 4 ,g/ml), ciprofloxacin (MICs, 0.5 to 8 ,ug/ml), and clindamycin (MICs, 0.25 to 64 ,g/ml. Both new quinolones were equally active against tetracyclinesusceptible as well as -resistant strains of M. hominis and U. urealyticum. The possible influence of medium components and/or pH on MICs was evaluated by testing a Staphylococcus aureus reference strain with each antibiotic in SP-4 broth and 10-B broth and comparing the results with published MICs for this strain. MICs determined in 10-B broth for erythromycin were affected most. This study shows that the activities of sparfloxacin and PD 127391 are similar to one another and comparable or superior to those of other drugs used to treat mycoplasmal infections. The MICs of both new quinolones were consistently 2 to several dilutions lower than those of ciprofloxacin for each species.Mycoplasma pneumoniae has long been recognized as a common pulmonary pathogen, especially in younger age groups, causing as much as 20% of pneumonia in the general population and up to 50% in military settings (3). Most respiratory infections due to M. pneumoniae are self-limiting, but in some instances life-threatening disease may occur (3). Although naturally occurring strains of M. pneumoniae resistant to erythromycin have not been described to date, the effectiveness of this drug may be limited in some cases because of dose-related nausea, vomiting, or diarrhea, justifying the need for alternative treatment modalities (9). Knowledge of the antibiotic susceptibilities of Mycoplasma hominis and Ureaplasma urealyticum is of increasing importance because of the recognition of these organisms as opportunistic pathogens in newborn infants (4-6, 42, 45) and other immunosuppressed persons (36) and as primary pathogens in sexually transmitted diseases such as nongonococcal urethritis (5) and pelvic inflammatory disease (5). Resistance to traditional drugs such as tetracycline, which has ...