scholarly journals Comparative Antimicrobial Activities of the Newly Synthesized Quinolone WQ-3034, Levofloxacin, Sparfloxacin, and Ciprofloxacin against Mycobacterium tuberculosis andMycobacterium avium Complex

2000 ◽  
Vol 44 (2) ◽  
pp. 283-286 ◽  
Author(s):  
Haruaki Tomioka ◽  
Katsumasa Sato ◽  
Hiroko Kajitani ◽  
Tatsuya Akaki ◽  
Shinji Shishido

ABSTRACT WQ-3034 is a newly synthesized acidic fluoroquinolone. We assessed its in vitro activity against Mycobacterium tuberculosisand M. avium complex using levofloxacin (LVFX), ciprofloxacin (CPFX), sparfloxacin (SPFX), and KRM-1648 (KRM) as reference drugs. The MICs of these agents were determined by the agar dilution method with 7H11 medium. The MICs at which 50 and 90% of the test strains were inhibited (MIC50s, and MIC90s, respectively) for the test quinolones for rifampin (RMP)-susceptible M. tuberculosis strains were in the order SPFX < LVFX ≦ WQ-3034 ≦ CPFX, while those for RMP-resistant M. tuberculosis strains were in the order SPFX ≦ WQ-3034 ≦ LVFX < CPFX. The MICs of KRM for RMP-susceptible M. tuberculosis were much lower than those of the test quinolones, while the MIC90 of KRM for RMP-resistant M. tuberculosis strains was higher than those of the quinolones. The MIC50s and MIC90s of the test drugs for M. avium were in the order KRM < SPFX < CPFX ≦ WQ-3034 ≦ LVFX, while those forM. intracellulare were in the order KRM < SPFX < WQ-3034 ≒ LVFX ≦ CPFX. Next, we compared the antimicrobial activities of the test drugs against M. tuberculosisorganisms residing in cells of the Mono Mac 6 macrophage (Mφ)-like cell line (MM6-Mφs) and of the A-549 type II alveolar cell line (A-549 cells). When drugs were added at the concentration that achieves the maximum concentration in blood, progressive killing or inhibition of the M. tuberculosis organisms residing in MM6-Mφs and A-549 cells was observed in the order KRM > SPFX ≧ LVFX > WQ-3034 > CPFX. The efficacies of all quinolones against intracellular M. tuberculosis organisms were significantly lower in A-549 cells than in MM6-Mφs. WQ-3034 at the MIC caused more marked growth inhibition of intramacrophage M. tuberculosis than did LVFX. These findings indicate that the in vitro anti-M. tuberculosis activity of WQ-3034 is greater than that of CPFX and is comparable to that of LVFX.

2003 ◽  
Vol 47 (11) ◽  
pp. 3667-3671 ◽  
Author(s):  
A. Liebetrau ◽  
A. C. Rodloff ◽  
J. Behra-Miellet ◽  
L. Dubreuil

ABSTRACT The antimicrobial activities of garenoxacin and eight other antibiotics against 641 anaerobic isolates were evaluated with the NCCLS agar dilution method. Overall, the MICs of garenoxacin for 50 and 90% of the strains tested (in micrograms per milliliter) were as follows: Bacteroides fragilis group, 0.5 and 2; Prevotella spp., 0.25 and 2; Fusobacterium spp., 0.25 and 0.5; Porphyromonas spp., 0.125 and 0.25; Bilophila wadsworthia, 0.5 and 1; Veillonella spp., 0.25 and 0.5; Clostridium spp., 0.25 and 1; Clostridium difficile, 2 and >64; Bifidobacterium spp., 1 and 2; Eggerthella lenta, 0.25 and 1; Propionibacterium spp., 0.5 and 0.5; gram-positive cocci, 0.125 and 0.25.


2007 ◽  
Vol 56 (11) ◽  
pp. 1490-1494 ◽  
Author(s):  
Malini R. Capoor ◽  
Deepti Rawat ◽  
Deepthi Nair ◽  
Azra S. Hasan ◽  
Monorama Deb ◽  
...  

The therapeutic alternatives available for use against ciprofloxacin-resistant enteric fever isolates in an endemic area are limited. The antibiotics currently available are the quinolones, third-generation cephalosporins and conventional first-line drugs. In this study, the MICs of various newer drugs were determined for 31 ciprofloxacin-resistant enteric fever isolates (26 Salmonella enterica serovar Typhi and 5 S. enterica serovar Paratyphi A). MICs for ciprofloxacin, ofloxacin, gatifloxacin, levofloxacin, cefotaxime, cefixime, cefepime and azithromycin were determined using Etest strips and the agar dilution method. By Etest, all of the ciprofloxacin-resistant isolates had ciprofloxacin MICs ≥32 μg ml−1. S. Typhi showed MIC90 values of 0.50, 0.25 and 0.38 μg ml−1 for cefixime, cefotaxime and cefepime, respectively. For the cephalosporins, a negligible difference in MIC90 and MIC50 values for S. Typhi and S. Paratyphi A was observed. A single isolate of S. Typhi showed a high azithromycin MIC of 64 μg ml−1. The MIC90 value for azithromycin in S. Typhi and S. Paratyphi was 24 μg ml−1. Gatifloxacin demonstrated lower resistance (80.8 %) compared with the other quinolones (92–100 %) in S. Typhi. The rise in MIC levels of these antimicrobials is a matter for serious concern.


2006 ◽  
Vol 50 (1) ◽  
pp. 148-155 ◽  
Author(s):  
Ellie J. C. Goldstein ◽  
Diane M. Citron ◽  
Yumi A. Warren ◽  
Kerin L. Tyrrell ◽  
C. Vreni Merriam ◽  
...  

ABSTRACT The in vitro activity of moxifloxacin against 923 recent anaerobic isolates obtained from pretreatment cultures in patients with complicated intra-abdominal infections was studied using the CLSI M11-A-6 agar dilution method. Moxifloxacin was active against 87% (96 of 110) Bacteroides fragilis strains at ≤1 μg/ml and 87% (79 of 90) B. thetaiotaomicron strains at ≤2 μg/ml. Species variation was seen, with B. uniformis, B. vulgatus, Clostridium clostridioforme, and C. symbiosum being least susceptible and accounting for most of the resistant isolates; excluding the aforementioned four resistant species, 86% (303 of 363) of Bacteroides species isolates and 94% (417 of 450) of all other genera and species were susceptible to ≤2 μg/ml of moxifloxacin. Overall, moxifloxacin was active against 763 of 923 (83%) of strains at ≤2 μg/ml, supporting its use as a monotherapy for some community-acquired intra-abdominal infections.


1997 ◽  
Vol 41 (4) ◽  
pp. 841-843 ◽  
Author(s):  
S A Radford ◽  
E M Johnson ◽  
D W Warnock

The in vitro activity of voriconazole was compared with that of itraconazole. Eighty-six isolates of pathogenic molds belonging to 23 species were tested by an agar dilution method in High Resolution medium. Voriconazole was more active than itraconazole against a number of hyaline molds, including several Fusarium spp. and Scedosporium prolificans. Voriconazole and itraconazole showed comparable good activity against several hyaline molds, including Penicillium marneffei and Scedosporium apiospermum, and a number of dematiaceous molds, including Bipolaris australiensis, Cladophialophora bantiana, several Exophiala spp., and several Fonsecaea spp. Our results suggest that voriconazole could be effective against a wide range of mold infections in humans.


2006 ◽  
Vol 50 (1) ◽  
pp. 379-381 ◽  
Author(s):  
Ellie J. C. Goldstein ◽  
Diane M. Citron ◽  
C. Vreni Merriam ◽  
Yumi A. Warren ◽  
Kerin L. Tyrrell ◽  
...  

ABSTRACT Using the NCCLS agar dilution method, we studied the in vitro activity of retapamulin (SB-275833) against 141 clinical isolates of Propionibacterium species, including seven multiresistant strains, and found retapamulin to be the most active agent among those tested with MICs of ≤1 μg/ml against all isolates.


2006 ◽  
Vol 50 (8) ◽  
pp. 2728-2731 ◽  
Author(s):  
Kerin L. Tyrrell ◽  
Diane M. Citron ◽  
Yumi A. Warren ◽  
Helen T. Fernandez ◽  
C. Vreni Merriam ◽  
...  

ABSTRACT Daptomycin has in vitro activity against gram-positive anaerobic bacteria, although limited numbers of species have been tested. We studied the in vitro activities of daptomycin, vancomycin, and penicillin against more than 100 strains each of Clostridium difficile, C. perfringens, Finegoldia magna, and Propionibacterium acnes. Daptomycin Etest MICs and results from time-kill studies were determined for selected strains. For 392 of 421 strains (93%), daptomycin was inhibitory at ≤1 μg/ml, including 15 of 16 strains of C. difficile with elevated linezolid MICs of 8 and 16 μg/ml, all 32 strains with moxifloxacin MICs of ≥4 μg/ml, and all 16 strains resistant to clindamycin. Daptomycin MICs were also ≤1 μg/ml for all 16 F. magna strains resistant to clindamycin and all 32 strains resistant to tetracycline. Only one strain, a C. perfringens strain, had a MIC of >2 μg/ml to daptomycin. Eighty-five and 92.5% of the Etest MICs were within 1 dilution of the agar dilution method for all drugs at 24 and 48 h, respectively. In time-kill studies, a C. difficile strain was inhibited by both daptomycin and vancomycin at 1, 2, 4, 8, and 24 h; colony counts were decreased by 2.3 to 2.9 log at 24 h. Vancomycin was not bactericidal for C. perfringens; however, daptomycin showed bactericidal activity as early as 1 h at four and eight times the MIC and at 2 and 4 h at two and four times the MIC.


2018 ◽  
Vol 20 (3) ◽  
pp. 192-197
Author(s):  
Natalya N. Dekhnich ◽  
Nataly V. Ivanchik ◽  
Roman S. Kozlov

Objective. Compare the in vitro activity of clarithromycin, erythromycin, azithromycin and josamycin against the collection of H. pylori strains isolated in 2010–2017 in Smolensk. Materials and Methods. H. pylori strains were collected prospectively from biopsy specimens of the gastric mucosa. Antimicrobial susceptibility testing of H. pylori was performed by the agar dilution method. Interpretation of the results of the susceptibility determination for clarithromycin was carried out in accordance with the recommendations of EUCAST (v 8.0) 2018. The resistance breakpoints for erythromycin, azithromycin, and josamycin were all set at ≥1.0 mg/L. For comparison of the results, the value of the minimal inhibitory concentrations of the tested antibiotic inhibiting the growth of 50% (MIC50) and 90% (MIC90) of H. pylori strains was used. Results. A total of 276 H. pylori strains were tested. 90% of the MIC values of clarithromycin were in the range from 0.015 to 0.125 mg/l. The percentages of resistance were as follows: clarithromycin 5.1%, azithromycin 7.5%, erythromycin 8%, josamycin 23.2%. Clarithromycin demonstrated significantly higher activity in suppressing the growth of H. pylori strains than azithromycin, erythromycin, and josamycin. Conclusions. Among the tested macrolide antibiotics maximal anti-H. pylori activity in vitro was observed in clarithromycin.


2019 ◽  
Vol 15 (3) ◽  
pp. 257-264 ◽  
Author(s):  
Fatma Boukattaya ◽  
Amal Daoud ◽  
Fabien Boeda ◽  
Morwenna S.M. Pearson-Long ◽  
Néji Gharsallah ◽  
...  

Background: 2-Aminochromene derivatives display important pharmacological properties, including mainly antibiotic and anticancer activities. Objective: The study aims to synthesize new chromene derivatives via a new approach using Grignard reagents, for the evaluation of their antibiotic and antifungal properties. Method: A series of novel 3-cyano-4-aminochromene derivatives bearing alkyl substituents at the 4-position was prepared for biological evaluation. Results: These compounds were obtained by the addition of various Grignard reagents into Nethoxycarbonyl- 3-cyanoiminocoumarines in moderate to good yields (72-96%). The reaction is completely regioselective. The new chromene derivatives were screened for their in vitro antimicrobial activities against a panel of six bacterial and three fungal strains using agar dilution method. Conclusion: The antibacterial activity of the chromene derivatives was more pronounced on Gram-positive bacteria than on Gram-negative bacteria with a significant activity observed against Staphylococcus aureus. An interesting antifungal activity against Fusarium sp. and Fusarium oxysporum was also noticed.


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