Activity of BAY y 3118, a Novel 4-Quinolone, against<i>Brucella melitensis</i>

Garcı́a-Rodrı́guez, J.A.; Garcı́a-Sánchez, José Elı́as; Trujillano-Martín, I.; Garcı́a-Sánchez, Enrique; García-Garcia, M I; Fresnadillo, Ma.J.

doi:10.1080/1120009x.1994.11741137

Cited by 4 publications

(1 citation statement)

References 18 publications

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“…Most studies that examined the use of quinolones against B. melitensis showed, generally, low MICs values; where the MIC 90 to the ofloxacin was 0.02–2.5 mg/l (11, 14, 17); to the levofloxacin 0.5 mg/l (17, 28); to the sparfloxacin 0.12–2 mg/l (11, 12, 26); to the ciprofloxacin 0.06–2 mg/l (7, 17, 19); and to the moxifloxacin 0.5–1 mg/l (19, 28). However, among the quinolones that are used in our study, ciprofloxacin revealed the lowest MIC range against the isolates collected from all Syrian regions (MIC range 0.07–6.25 μg/ml), and moxifloxacin showed the highest MIC range (MIC range 1.5–100 μg/ml).…”

Section: Discussionmentioning

confidence: 99%

Efficacy evaluation of some antibiotics against syrian brucella spp isolates, in vitro

Safi

Al-Mariri

2012

Braz. J. Microbiol.

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Brucellosis is an endemic zoonosis in Syria, affecting large numbers of animals and there are an increasing number of cases in humans. The aim of this study is to investigate the in vitro efficacy of various traditional and new antibiotics against 89 Brucella isolates (isolated from domestic animals) collected from different Syrian regions. Minimum inhibitory concentrations (MICs) of seventeen antibiotics were determined. Ciprofloxacin and ofloxacin were the most effective antibiotics, whereas sparfloxacin, levofloxacin, doxycycline and tetracycline had a moderate activity. In contrast, moxifloxacin and rifampicin had a low activity, while streptomycin, spiramycin and cephalosporines were ineffective. As a result, we come to the conclusion that a combination between one effective quinolone and doxycycline has a good efficacy against Brucella. Further in vivo studies are necessary to support this suggestion.

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Section: Discussionmentioning

confidence: 99%

Efficacy evaluation of some antibiotics against syrian brucella spp isolates, in vitro

Safi

Al-Mariri

2012

Braz. J. Microbiol.

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Antibrucella Activity of Quinolone Sparfloxacin

et al. 1995

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Background: Sparfloxacin is a new fluoroquinolone with excellent in vitro activity against a variety of Gram-positive and Gram-negative bacteria. Methods: In vitro antibacterial activity of this new drug was tested against 139 strains of Brucella melitensis. These strains were isolated from 138 patients at a major tertiary care referral center in Riyadh, Saudi Arabia. Results: Seven percent of the strains were inhibited by 0.06 mg per L and 99% by 0.12 mg per L of sparfloxacin. Of the five other fluoroquinolones tested, ciprofloxacin, norfloxacin, pefloxacin, and fleroxacin exhibited comparable or slightly higher minimal inhibitory concentrations values. They inhibited the growth of 138 of the 139 isolates at 0.25-0.5 mg per L. Rufloxacin required 2-8 mg per L to inhibit 138 of the 139 strains tested. One of the isolates, which had previously developed resistance to ciprofloxacin during therapy with this drug, with a rise in MIC from 0.06 mg per L to >5.0 mg per L, exhibited cross-resistance to sparfloxacin and other fluoroquinolones. Conclusion: Sparfloxacin exhibited excellent in vitro activity against clinical isolates of Brucella. Clinical trials are warranted to determine its potential in the treatment of brucellosis.

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Susceptibilities of Brucella melitensis isolates to clinafloxacin and four other new fluoroquinolones

Garcı́a-Rodrı́guez

Sánchez

Trujillano

et al. 1995

Antimicrob Agents Chemother

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The susceptibilities of 120 clinical isolates of Brucella melitensis and 3 reference strains of the same species to six fluoroquinolones (clinafloxacin, PD 117596, PD 131628, PD 138312, PD 140248, and ciprofloxacin) were examined by agar dilution MIC methodology. Clinafloxacin was the most active compound tested (MIC at which 50% of strains tested were inhibited [MIC 50 ] and MIC 90 of 0.06 g/ml). Its level of activity was slightly higher than that of PD 117596 (MIC 50 and MIC 90 of 0.12 g/ml). PD 131628 and ciprofloxacin were less active than clinafloxacin, with MIC 50 s ranging from 0.12 to 0.25 g/ml and MIC 90 s of between 0.25 and 0.5 g/ml for the two compounds. The activity levels of PD 138312 and PD 140248, with MIC 50 s ranging from 1 to 2 g/ml and MIC 90 s of 4 to 8 g/ml, were lower than those of the other fluoroquinolones tested.Brucellosis remains a public health problem in several areas, such as Mediterranean countries. The treatment of brucellosis requires combined regimens of antibiotics and is conditioned by the fact that Brucella species are intracellular pathogens; thus, agents with a good capacity to penetrate macrophages are required for successful treatment. Current treatment of acute brucellosis combining tetracyclines and streptomycin or rifampin usually achieves excellent clinical and microbiological results. Nevertheless, variable percentages of failures and recurrences, ranging from 4 to 41% depending on the therapeutic regimens, are reported (1). In addition, these therapeutic regimens pose difficulties in patients' compliance because of their duration; moreover, tetracyclines are contraindicated for children of less than 8 years old and for pregnant women. Furthermore, since the incidence of tuberculosis in some areas of the world is increasing, the use of rifampin for nontuberculous patients in these areas should be avoided. Thus, it is felt that new antibiotics overcoming these problems would represent a significant therapeutic advancement in the treatment of brucellosis.Oral bioavailability of fluoroquinolones, high concentrations in tissues, evidence of intracellular penetration (leukocytes and macrophages) (5), and in vitro activity against Brucella spp. (7, 9) make these antimicrobial agents attractive for use against infections caused by intracellular bacteria such as Brucella spp. However, agents currently available in clinical practice (ciprofloxacin, ofloxacin, lomefloxacin, fleroxacin, and sparfloxacin) have moderate activity and lack effective bactericidal activity under intracellular conditions (pH 5) (7-9). Moreover, therapeutic failures caused by the development of resistance to these agents by Brucella melitensis have also been reported (3). Therefore, these fluoroquinolones should not be considered for primary treatment of brucellosis. Thus, it is important to evaluate new fluoroquinolones with higher intrinsic activity levels that might overcome these problems. Clinafloxacin The MICs of the antimicrobial agents were determined by the agar dilution method by using prev...

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Activity of BAY y 3118, a Novel 4-Quinolone, againstBrucella melitensis

Cited by 4 publications

References 18 publications

Efficacy evaluation of some antibiotics against syrian brucella spp isolates, in vitro

Efficacy evaluation of some antibiotics against syrian brucella spp isolates, in vitro

Antibrucella Activity of Quinolone Sparfloxacin

Susceptibilities of Brucella melitensis isolates to clinafloxacin and four other new fluoroquinolones

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