scholarly journals In Vitro Antibacterial Potency and Spectrum of ABT-492, a New Fluoroquinolone

2003 ◽  
Vol 47 (10) ◽  
pp. 3260-3269 ◽  
Author(s):  
Angela M. Nilius ◽  
Linus L. Shen ◽  
Dena Hensey-Rudloff ◽  
Laurel S. Almer ◽  
Jill M. Beyer ◽  
...  

ABSTRACT ABT-492 demonstrated potent antibacterial activity against most quinolone-susceptible pathogens. The rank order of potency was ABT-492 > trovafloxacin > levofloxacin > ciprofloxacin against quinolone-susceptible staphylococci, streptococci, and enterococci. ABT-492 had activity comparable to those of trovafloxacin, levofloxacin, and ciprofloxacin against seven species of quinolone-susceptible members of the family Enterobacteriaceae, although it was less active than the comparators against Citrobacter freundii and Serratia marcescens. The activity of ABT-492 was greater than those of the comparators against fastidious gram-negative species, including Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, and Legionella spp. and against Pseudomonas aeruginosa and Helicobacter pylori. ABT-492 was as active as trovafloxacin against Chlamydia trachomatis, indicating good intracellular penetration and antibacterial activity. In particular, ABT-492 was more active than trovafloxacin and levofloxacin against multidrug-resistant Streptococcus pneumoniae, including strains resistant to penicillin and macrolides, and H. influenzae, including β-lactam-resistant strains. It retained greater in vitro activity than the comparators against S. pneumoniae and H. influenzae strains resistant to other quinolones due to amino acid alterations in the quinolone resistance-determining regions of the target topoisomerases. ABT-492 was a potent inhibitor of bacterial topoisomerases, and unlike the comparators, DNA gyrase and topoisomerase IV from either Staphylococcus aureus or Escherichia coli were almost equally sensitive to ABT-492. The profile of ABT-492 suggested that it may be a useful agent for the treatment of community-acquired respiratory tract infections, as well as infections of the urinary tract, bloodstream, and skin and skin structure and nosocomial lung infections.

1987 ◽  
Vol 8 (6) ◽  
pp. 241-244 ◽  
Author(s):  
Maury E. Mulligan ◽  
Y.Y. Kwok

AbstractCefixime, a broad-spectrum, orally active cephalosporin, was more active in vitro than ampicillin, cefaclor, cephalothin, and trimethoprim/sulfamethoxazole against 194 nosocomial pathogens of the family Enterobacteriaceae. Activity was especially good against Klebsiella spp, Proteus spp, Serratia spp, and Providencia stuartii. Although gentamicin had equivalent or better activity against Citrobacter spp, Enterobacter spp, Escherichia coli, and Morganella morganii, all 23 of the gentamicin-resistant strains studied were susceptible to Cefixime. Isolates tested were from urinary tract infections, abdominal infections, wounds, vascular infections, and respiratory infections; they were sequentially collected nosocomial pathogens from a single institution. This orally active cephalosporin should be considered for therapy of a variety of nosocomial infections involving gram-negative bacillary pathogens.


2008 ◽  
Vol 52 (3) ◽  
pp. 1182-1183 ◽  
Author(s):  
W. T. M. Jansen ◽  
A. Verel ◽  
J. Verhoef ◽  
D. Milatovic

ABSTRACT We investigated the in vitro activity of AR-709, a novel diaminopyrimidine antibiotic currently in development for treatment of community-acquired upper and lower respiratory tract infections, against 151 Streptococcus pneumoniae strains from various European countries. AR-709 showed excellent activity against both drug-susceptible and multidrug-resistant pneumococci.


Antibiotics ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 29 ◽  
Author(s):  
Larbi Zakaria Nabti ◽  
Farida Sahli ◽  
Hocine Laouar ◽  
Ahmed Olowo-okere ◽  
Joice Guileine Nkuimi Wandjou ◽  
...  

Antibiotics are becoming ineffective against resistant bacteria. The use of essential oils (EOs) may constitute an alternative solution to fight against multidrug-resistant bacteria. This study aims to determine the chemical composition of EOs from five populations of the endemic Algerian Origanum glandulosum Desf. and to investigate their potential antibacterial activity against multidrug-resistant uropathogenic E. coli strains. The EOs were obtained by hydrodistillation and their composition was investigated by gas chromatography/mass spectrometry (GC/MS). The antibacterial activity was evaluated by the disc diffusion method against eight E. coli strains (six uropathogenic resistant and two referenced susceptible strains). Minimum inhibitory and bactericidal concentrations (MIC/MBC) were obtained by the broth microdilution method. The main EO components were thymol (15.2–56.4%), carvacrol (2.8–59.6%), γ-terpinene (9.9–21.8%) and p-cymene (8.5–13.9%). The antibacterial tests showed that all the EOs were active against all the strains, including the multidrug-resistant strains. The EO from the Bordj location, which contained the highest amount of carvacrol (59.6%), showed the highest antibacterial activity (inhibition diameters from 12 to 24.5 mm at a dilution of 1/10). To our knowledge, this is the first description of the activity of O. glandulosum EOs against resistant uropathogenic strains. Our study suggests that O. glandulosum EO could be used in some clinical situations to treat or prevent infections (e.g., urinary tract infections) with multidrug-resistant strains.


Marine Drugs ◽  
2018 ◽  
Vol 16 (8) ◽  
pp. 289 ◽  
Author(s):  
Decha Kumla ◽  
José Pereira ◽  
Tida Dethoup ◽  
Luis Gales ◽  
Joana Freitas-Silva ◽  
...  

A previously unreported chromene derivative, 1-hydroxy-12-methoxycitromycin (1c), and four previously undescribed chromone derivatives, including pyanochromone (3b), spirofuranochromone (4), 7-hydroxy-6-methoxy-4-oxo-3-[(1E)-3-oxobut-1-en-1-yl]-4H-chromene-5-carboxylic acid (5), a pyranochromone dimer (6) were isolated, together with thirteen known compounds: β-sitostenone, ergosterol 5,8-endoperoxide, citromycin (1a), 12-methoxycitromycin (1b), myxotrichin D (1d), 12-methoxycitromycetin (1e), anhydrofulvic acid (2a), myxotrichin C (2b), penialidin D (2c), penialidin F (3a), SPF-3059-30 (7), GKK1032B (8) and secalonic acid A (9), from cultures of the marine sponge- associated fungus Penicillium erubescens KUFA0220. Compounds 1a–e, 2a, 3a, 4, 7–9, were tested for their antibacterial activity against Gram-positive and Gram-negative reference and multidrug-resistant strains isolated from the environment. Only 8 exhibited an in vitro growth inhibition of all Gram-positive bacteria whereas 9 showed growth inhibition of methicillin-resistant Staphyllococus aureus (MRSA). None of the compounds were active against Gram-negative bacteria tested.


2021 ◽  
Vol 16 (6) ◽  
pp. 409-420
Author(s):  
Sadaf Areej ◽  
Adeel Sattar ◽  
Aqeel Javeed ◽  
Sohail Raza

Background: Antibiotics are in use since decades to treat various infections caused by Gram-positive and Gram-negative bacteria such as Staphylococcus aureus and Pseudomonas aeruginosa. Diphenhydramine, an H1 receptor blocker possesses a weak antibiotic action but when combined with other antibiotics may potentiate their antibacterial activity. Materials & methods: This study investigated in vitro antibacterial activity of diphenhydramine when used alone and in combination with levofloxacin against methicillin-resistant S. aureus and P. aeruginosa. Results: The combined antibacterial effect of the drugs against bacteria showed a fractional inhibitory concentration index of ≤0.5, in other words, synergism. No cytotoxicity was observed as percentage cell viability was >50%. Conclusion: The combination of diphenhydramine and levofloxacin exerted antibacterial activity, and was not found to be cytotoxic when given in combination against P. aeruginosa and S. aureus.


2021 ◽  
Vol 22 (10) ◽  
Author(s):  
Muhammad Evy Prastiyanto

Abstract. Prastiyanto ME. 2021. Seeds extract of three Artocarpus species: Their in-vitro antibacterial activities against multidrug-resistant (MDR) Escherichia coli isolates from urinary tract infections (UTIs). Biodiversitas 22: 4362-4368. Multidrug-resistant (MDR)-E. coli is a major cause and has become a very serious problem in urinary tract infections (UTIs). As a result, it requires an antibacterial agent derived from biological materials. It has been reported that the seeds of three species of Artocarpus (A. heterophyllous, A. champeden, and A. camansi) have antibacterial properties against Methicillin-Resistant Staphylococcus aureus (MRSA). However, there are three other Artocarpus species in Indonesia, i.e., keledang (A. lanceipolius), tarra (A. elasticus), and terap (A. Odoratissimus) whose antibacterial property has not been investigated. To minimize the research gap, this study aims to determine the antibacterial activity of seed extracts of A. lanceipolius, A. elasticus, and A. odoratissimus against MDR-E. coli isolates of UTIs. Antibacterial activity was evaluated using the agar well diffusion assay. The microdilution method was used to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values. The results revealed that the seed extracts of A. lanceipolius, A. elasticus, and A. odoratissimus have the potential as antibacterial agents against MDR-E. coli isolate of UTIs. A. elasticus seed extract shows the widest zone of inhibition in the range of 7.0-13.3 mm and the smallest MIC and MBC values ??of 6.25-12.5 mg/mL and 12.5-25 mg/mL, respectively. In conclusion, A. lanceipolius, A. elasticus, and A. odoratissimus seed extracts have the potential to be developed as antibacterial agents against UTI-causing MDR-E. coli. Further in vivo research and determining the mode of action of antibacterial activity are needed.


2005 ◽  
Vol 49 (3) ◽  
pp. 889-894 ◽  
Author(s):  
Reiko Kobayashi ◽  
Mami Konomi ◽  
Keiko Hasegawa ◽  
Miyuki Morozumi ◽  
Keisuke Sunakawa ◽  
...  

ABSTRACT The in vitro activity of tebipenem (TBM), a new oral carbapenem antibiotic, against Streptococcus pneumoniae clinical isolates (n = 202) was compared with those of 15 reference agents. The isolates were classified into five genotypic classes after PCR identification of abnormal pbp1a, pbp2x, and pbp2b genes: (i) penicillin-susceptible S. pneumoniae (PSSP) isolates with no abnormal pbp genes (n = 34; 16.8%), (ii) genotypic penicillin-intermediate S. pneumoniae (gPISP) isolates with only an abnormal pbp2x gene [gPISP (2x)] (n = 48; 23.8%), (iii) gPISP isolates with abnormal pbp1a and pbp2x genes (n = 32; 15.8%), (iv) gPISP isolates with abnormal pbp2x and pbp2b genes (n = 16; 7.9%), and (v) genotypic penicillin-resistant S. pneumoniae (gPRSP) isolates with three abnormal pbp genes (n = 72; 35.6%). The majority of the strains tested had mefA (n = 59; 29.2%) or ermB (n = 91; 45%) gene-mediating macrolide resistance. For these isolates the MIC at which 90% of isolates are inhibited was significantly lower for TBM than for the reference oral antibiotics, as follows: 0.002 μg/ml for PSSP, 0.004 μg/ml for gPISP (2x), 0.016 μg/ml for gPISP (isolates with abnormal pbp1a and pbp2x genes and isolates with abnormal pbp2x and pbp2b genes), and 0.063 μg/ml for gPRSP. In addition, TBM showed excellent bactericidal activity against gPRSP isolates, which exhibited a 3-log10 decrease within 2 h when they were incubated with a concentration greater than or equal to the MIC. Inhibition of cell wall synthesis toward the long axis and subsequent cell lysis were observed by scanning electron microscopy after a short-term exposure to TBM, unlike the effects seen with cephalosporins. These data suggest that TBM has potent activity against multidrug-resistant S. pneumoniae, the causative pathogen of community-acquired respiratory tract infections.


Antibiotics ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 825
Author(s):  
Henrique Pinto ◽  
Manuel Simões ◽  
Anabela Borges

This study sought to assess the prevalence and impact of biofilms on two commonly biofilm-related infections, bloodstream and urinary tract infections (BSI and UTI). Separated systematic reviews and meta-analyses of observational studies were carried out in PubMed and Web of Sciences databases from January 2005 to May 2020, following PRISMA protocols. Studies were selected according to specific and defined inclusion/exclusion criteria. The obtained outcomes were grouped into biofilm production (BFP) prevalence, BFP in resistant vs. susceptible strains, persistent vs. non-persistent BSI, survivor vs. non-survivor patients with BSI, and catheter-associated UTI (CAUTI) vs. non-CAUTI. Single-arm and two-arm analyses were conducted for data analysis. In vitro BFP in BSI was highly related to resistant strains (odds ratio-OR: 2.68; 95% confidence intervals-CI: 1.60–4.47; p < 0.01), especially for methicillin-resistant Staphylococci. BFP was also highly linked to BSI persistence (OR: 2.65; 95% CI: 1.28–5.48; p < 0.01) and even to mortality (OR: 2.05; 95% CI: 1.53–2.74; p < 0.01). Candida spp. was the microorganism group where the highest associations were observed. Biofilms seem to impact Candida BSI independently from clinical differences, including treatment interventions. Regarding UTI, multi-drug resistant and extended-spectrum β-lactamase-producing strains of Escherichia coli, were linked to a great BFP prevalence (OR: 2.92; 95% CI: 1.30–6.54; p < 0.01 and OR: 2.80; 95% CI: 1.33–5.86; p < 0.01). More in vitro BFP was shown in CAUTI compared to non-CAUTI, but with less statistical confidence (OR: 2.61; 95% CI: 0.67–10.17; p < 0.17). This study highlights that biofilms must be recognized as a BSI and UTI resistance factor as well as a BSI virulence factor.


2020 ◽  
Vol 7 (Supplement_1) ◽  
pp. S655-S655
Author(s):  
Daniel Navas ◽  
Angela Charles ◽  
Amy Carr ◽  
Jose Alexander

Abstract Background The activity of imipenem/relebactam (I/R), ceftazidime/avibactam (CZA) and cefiderocol (FDC) were evaluated against clinical isolates of multidrug resistant (MDR) strains of P. aeruginosa which was resistant to ceftolozane/tazobactam (C/T). The recent increase of MDR P. aeruginosa strains isolated from clinical samples has prompted research and development of new antimicrobials that can withstand its multiple resistance mechanisms. C/T is an effective option for treatment of MDR P. aeruginosa in our facility with only 10% of resistance in MDR strains, but the emergence of resistance may occur due to the presence of a carbapenemase gene or an ampC mutation. Methods Antimicrobial susceptibility testing for C/T Etest® (bioMérieux, Inc.) were performed on all MDR strains initially screened by the VITEK2® (bioMérieux, Inc.). 10% (n=20) of all MDR isolates were resistant to C/T by the CLSI 2019 breakpoints. These resistant isolates were tested for presence of a carbapenemase gene using the GeneXpert CARBA-R (Cepheid®) PCR and against CZA Etest® (bioMérieux, Inc.) I/R gradient strips (Liofilchem®) and FDC broth microdilution (Thermo Scientific™ Sensititre™). Results A total of 20 clinical isolates of MDR P. aeruginosa resistant to C/T were tested following standardized CLSI protocols and techniques. All 20 isolates were screened for the presence of a carbapenemase gene (blaVIM, blaNDM, blaKPC, blaOXA-48, blaIMP). A blaVIM gene was detected in 6 (30%) out of 20 isolates. FDC demonstrated the greatest activity with 85% (n=17) of susceptible isolates (CLSI MIC &lt;4µg/dL). CZA (CLSI MIC &lt;8µg/dL) and I/R (FDA MIC &lt;2µg/dL) showed 15% (n=3) and 10% (n=2) of susceptible isolates respectively. FDC was active against all 6 blaVIM isolates, where all 6 strains were resistant to CZA and I/R as expected. 3 isolates tested non-susceptible against FDC; additional characterization was not performed at this time. Conclusion Based on these results, FDC demonstrated the greatest in-vitro activity against C/T resistant strains of MDR P. aeruginosa. FDC also demonstrated activity against all 6 MDR P. aeruginosa carrying blaVIM gene. FDC is a strong option to consider on MDR P. aeruginosa strains based on a resistance testing algorithm and a cost/effective protocol. Disclosures All Authors: No reported disclosures


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