scholarly journals Activities of a New Oral Streptogramin, XRP 2868, Compared to Those of Other Agents against Streptococcus pneumoniae and Haemophilus Species

2003 ◽  
Vol 47 (10) ◽  
pp. 3270-3274 ◽  
Author(s):  
Glenn A. Pankuch ◽  
Linda M. Kelly ◽  
Gengrong Lin ◽  
Andre Bryskier ◽  
Catherine Couturier ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Streptococcus Pneumoniae ◽  
Haemophilus Influenzae ◽  
Antibacterial Agents ◽  
Penicillin G ◽  
Haemophilus Parainfluenzae ◽  
Haemophilus Species ◽  
Resistant Strains ◽  
Erythromycin A ◽  
Low Activity

ABSTRACT MIC methodology was used to test the antibacterial activity of XRP 2868, a new oral combination of two semisynthetic streptogramins, RPR 132552A and RPR 202868, compared to activities of other antibacterial agents against pneumococci, Haemophilus influenzae, and Haemophilus parainfluenzae. For 261 pneumococci, XRP 2868 and pristinamycin MICs were similar, irrespective of penicillin G and erythromycin A susceptibilities (MIC at which 50% of isolates were inhibited [MIC50], 0.25 μg/ml; MIC90, 0.5 μg/ml), while quinupristin/dalfopristin had MICs which were 1 to 2 dilutions higher. Single components of both XRP 2868 and quinupristin/dalfopristin had higher MICs. Erythromycin A, azithromycin, clarithromycin, and clindamycin MICs were higher for penicillin G-intermediate and -resistant than -susceptible pneumococci. Against 150 H. influenzae strains, all compounds tested had unimodal MIC distributions. XRP 2868 had an overall MIC50 of 0.25 μg/ml and an MIC90 of 1.0 μg/ml, with no differences between β-lactamase-positive, β-lactamase-negative, and β-lactamase-negative ampicillin-resistant strains. Of note was the similarly low activity of one of its components, RPR 132552A. Pristinamycin and quinupristin/dalfopristin had MICs of 0.125 to 8.0 μg/ml; quinupristin alone had MICs of 8.0 to >64.0 μg/ml, and dalfopristin had MICs of 1.0 to >64.0 μg/ml. Erythromycin A, azithromycin, and clarithromycin had modal MICs of 4.0, 1.0, and 8.0 μg/ml, respectively. MICs of all compounds against H. parainfluenzae were 1 to 2 dilutions higher than against H. influenzae. XRP 2868 showed potent activity against pneumococci and Haemophilus strains irrespective of their susceptibility to other agents.

scholarly journals In Vivo Efficacy of Telithromycin (HMR3647) againstStreptococcus pneumoniae and Haemophilus influenzae

2001 ◽  
Vol 45 (11) ◽  
pp. 3250-3252 ◽  
Author(s):  
Hiroki Okamoto ◽  
Shuichi Miyazaki ◽  
Kazuhiro Tateda ◽  
Yoshikazu Ishii ◽  
Keizo Yamaguchi
Keyword(s):  
Streptococcus Pneumoniae ◽  
Respiratory Tract ◽  
Haemophilus Influenzae ◽  
Respiratory Tract Infections ◽  
Penicillin G ◽  
In Vivo Efficacy ◽  
Erythromycin A ◽  
Tract Infections

ABSTRACT The in vivo activity of telithromycin against erythromycin A- and penicillin G-resistant Streptococcus pneumoniae was superior to that of azithromycin, clarithromycin, cefdinir, and levofloxacin. In respiratory tract infections caused by erythromycin A-susceptible S. pneumoniae or Haemophilus influenzae in mice, telithromycin was more effective than clarithromycin and comparable to azithromycin.

scholarly journals Antibacterial activity of RU 64004 (HMR 3004), a novel ketolide derivative active against respiratory pathogens.

1997 ◽  
Vol 41 (10) ◽  
pp. 2149-2158 ◽  
Author(s):  
C Agouridas ◽  
A Bonnefoy ◽  
J F Chantot
Keyword(s):  
Antibacterial Activity ◽  
Streptococcus Pyogenes ◽  
Respiratory Infections ◽  
Membered Ring ◽  
Penicillin G ◽  
Respiratory Pathogens ◽  
Bacterial Strains ◽  
Good Antibacterial Activity ◽  
Resistant Strains ◽  
Erythromycin A

The antibacterial activity of RU 64004, a new ketolide, was evaluated against more than 600 bacterial strains and was compared with those of various macrolides and pristinamycin. RU 64004 had good activity against multiresistant pneumococci, whether they were erythromycin A resistant or not, including penicillin-resistant strains. RU 64004 inhibited 90% of pneumococci resistant to erythromycin A and penicillin G at 0.6 and 0.15 microg/ml, respectively. Unlike macrolides, RU 64004 did not induce the phenotype of resistance to macrolides-lincosamides-streptogramin B. Its good antibacterial activity against multiresistant pneumococci ran in parallel with its well-balanced activity against all bacteria involved in respiratory infections (e.g., Haemophilus influenzae, Moraxella catarrhalis, Streptococcus pyogenes). In contrast to all comparators (14- and 16-membered-ring macrolides and pristinamycin), RU 64004 displayed high therapeutic activity in animals infected with all major strains, irrespective of the phenotypes of the strains. The results suggest that RU 64004 has potential for use in the treatment of infections caused by respiratory pathogens including multiresistant pneumococci.

Synthesis of Fluorinated Piperazinyl Substituted Quinazolines as Potential Antibacterial Agents

2020 ◽  
Vol 5 (3) ◽  
pp. 227-233
Author(s):  
Amit B. Patel ◽  
Purvesh Patel ◽  
Kajal Patel ◽  
Krupa Prajapati
Keyword(s):  
Antibacterial Activity ◽  
13C Nmr ◽  
Antibacterial Agents ◽  
Multidrug Resistant ◽  
Biological Species ◽  
Piperazine Ring ◽  
Minimum Inhibitory Concentrations ◽  
Ft Ir ◽  
Resistant Strains ◽  
Quinazoline Derivatives

In present study, fluorinated piperazine and benzonitrile/nicotinonitrile fused quinazoline derivatives have synthesized, characterized using FT-IR, 1H & 13C NMR, 19F NMR and MS analysis and evaluated as potential antibacterial agents. They were also tested against the multidrug resistant strains. The antibacterial activity results revealed that the majority of synthesized compounds exhibited potential antibacterial with the extraordinary level of minimum inhibitory concentrations comparable to the control drugs. Moreover, the influence of presence or absence of fluoro and trifluoromethyl functional groups on the piperazine ring systems towards different biological species is elaborated. The synthesized compounds were also found non-toxic on the human cervical (HeLa) cells at their minimum inhibitory concentrations.

scholarly journals Activity of LBM415 Compared to Those of 11 Other Agents against Haemophilus Species

2006 ◽  
Vol 50 (7) ◽  
pp. 2323-2329 ◽  
Author(s):  
Tatiana Bogdanovich ◽  
Kathy A. Smith ◽  
Catherine Clark ◽  
Glenn A. Pankuch ◽  
Gengrong Lin ◽  
...  
Keyword(s):  
Haemophilus Influenzae ◽  
Ribosomal Protein ◽  
Peptide Deformylase ◽  
Resistance Selection ◽  
Haemophilus Species ◽  
Resistant Strains ◽  
Resistant Mutants ◽  
Protein Mutations ◽  
Time Kill

ABSTRACT When tested against 254 Haemophilus influenzae strains, LBM415, a peptide deformylase inhibitor, gave MIC50 and MIC90 values of 2.0 μg/ml and 8.0 μg/ml, respectively. The MICs were independent of β-lactam or quinolone susceptibility and the presence or absence of macrolide efflux or ribosomal protein mutations. The MICs of LBM415 against 23 H. parainfluenzae strains were similar to those against H. influenzae. In contrast, erythromycin, azithromycin, and clarithromycin gave unimodal MIC distributions, and apart from β-lactamase-negative, ampicillin-resistant strains, all strains were susceptible to the β-lactams tested. Apart from selected quinolone-resistant strains, all strains were susceptible to ciprofloxacin, levofloxacin, gatifloxacin, moxifloxacin, and gemifloxacin. Resistance to trimethoprim-sulfamethoxazole was common. The potencies of all drugs against 23 H. parainfluenzae strains were similar to those against H. influenzae. Time-kill studies with 10 Haemophilus strains showed LBM415 to be bactericidal at 2× the MIC against 8 of 10 strains after 24 h. For comparison, the macrolides and β-lactams were bactericidal against 8 to 10 strains each at 2× the MIC after 24 h. Quinolones were bactericidal against all 10 strains tested at 2× the MIC after 24 h. Against six H. influenzae strains, postantibiotic effects for LBM415 lasted between 0.8 and 2.2 h. In multistep resistance selection studies, LBM415 produced resistant clones in 7 of the 10 strains tested, with MICs ranging from 4 to 64 μg/ml. No mutations in deformylase (def) and formyltransferase (fmt) genes were detected in any of the LBM415-resistant mutants.

scholarly journals In Vitro Activities of Novel 2-Fluoro-Naphthyridine-Containing Ketolides

2005 ◽  
Vol 49 (1) ◽  
pp. 309-315 ◽  
Author(s):  
Darren Abbanat ◽  
Glenda Webb ◽  
Barbara Foleno ◽  
Y. Li ◽  
Mark Macielag ◽  
...  
Keyword(s):  
Protein Synthesis ◽  
Streptococcus Pneumoniae ◽  
Respiratory Tract ◽  
Haemophilus Influenzae ◽  
Moraxella Catarrhalis ◽  
Bacterial Strains ◽  
Erythromycin A ◽  
Time Kill ◽  
Vitro Protein

ABSTRACT In vitro activities of erythromycin A, telithromycin, and two investigational ketolides, JNJ-17155437 and JNJ-17155528, were evaluated against clinical bacterial strains, including selected common respiratory tract pathogens. Against 46 macrolide-susceptible and -resistant Streptococcus pneumoniae strains, the MIC90 (MIC at which 90% of the isolates tested were inhibited) of the investigational ketolides was 0.25 μg/ml, twofold lower than that of telithromycin and at least 64-fold lower than that of erythromycin A. Against erm(B)-containing pneumococci, the MIC90 of all the ketolides was 0.06 μg/ml. The MIC90 of the investigational ketolides against mef(A)-containing pneumococci or pneumococci with both mef(A) and erm(B) was 0.25 μg/ml, two-and fourfold lower, respectively, than that of telithromycin. In contrast, the MICs of the investigational ketolides against macrolide-resistant S. pneumoniae strains with ribosomal mutations were similar to or, in some cases, as much as eightfold higher than those of telithromycin. Against Haemophilus influenzae, MICs of all the ketolides were ≤2 μg/ml. Against three Moraxella catarrhalis isolates, the MIC of the ketolides was 0.25 μg/ml. The ketolides inhibited in vitro protein synthesis, with 50% inhibitory concentrations ranging from 0.23 to 0.27 μM. In time-kill studies against macrolide-susceptible and erm- or mef-containing pneumococci, the ketolides were bacteriostatic to slowly bactericidal, with 24-h log10 decreases ranging from 2.0 to 4.1 CFU. Intervals of postantibiotic effects for the ketolides against macrolide-susceptible and -resistant S. pneumoniae were 3.0 to 8.1 h.

scholarly journals Postantibiotic Suppression of Growth of Erythromycin A-Susceptible and -Resistant Gram-Positive Bacteria by the Ketolides Telithromycin (HMR 3647) and HMR 3004

2000 ◽  
Vol 44 (6) ◽  
pp. 1749-1753 ◽  
Author(s):  
Wendy J. Munckhof ◽  
Glenn Borlace ◽  
John D. Turnidge
Keyword(s):  
Staphylococcus Aureus ◽  
Streptococcus Pneumoniae ◽  
Streptococcus Pyogenes ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Resistant Strains ◽  
Erythromycin A

ABSTRACT We investigated the in vitro postantibiotic effects (PAEs) of the ketolides telithromycin (HMR 3647) and HMR 3004 and analyzed the results using the sigmoid E max model. Mean maximum telithromycin PAEs against erythromycin A-susceptible strains of Staphylococcus aureus, Streptococcus pyogenes, and Streptococcus pneumoniae were 3.7, 8.9, and 9.7 h, respectively, while maximum PAEs for erythromycin A-resistant strains were much shorter. Mean maximum HMR 3004 PAEs were 3.2 to 4.4 h for all species.

scholarly journals Antibacterial Activity of Leaf Extracts of Anredera cordifolia (Ten.) Steenis and Muntingia calabura L. Against Streptococcus pneumoniae

2020 ◽  
Vol 7 (1) ◽  
pp. 1-9
Author(s):  
Nuke Annisa Nasution ◽  
I Made Artika ◽  
Dodi Safari
Keyword(s):  
Antibacterial Activity ◽  
Streptococcus Pneumoniae ◽  
Clinical Isolate ◽  
Antibacterial Agent ◽  
Antibacterial Agents ◽  
Leaf Extracts ◽  
Extract Concentration ◽  
Global Concern ◽  
Muntingia Calabura

Antibacterial resistance in Streptococcus pneumoniae has been increasing and is one of ongoing global concern.  The need to find new antibacterial agents against Streptococcus pneumoniae is of paramount importance. Medicinal plants are prospective sources of antibacterial agents. The aims of the present study were to determine the activity of leaf extraxt of Anredera cordifolia (Ten.) Steenis and Muntingia calabura L. against Streptococcus pneumoniae.  Leaves of Anredera cordifolia (Ten.) Steenis were extracted using 96% ethanol, while the leaves of Muntingia calabura L were extracted using 100% methanol.  The leaf extracts of the two plants obtained were bioassayed for antibacterial activity against Streptococcus pneumoniae ATCC 49619 and a clinical isolate Streptococcus pneumoniae PU 067.  Results showed that leaf extracts of both Anredera cordifolia (Ten.) Steenis and Muntingia calabura L. have antibacterial activity in vitro against Streptococcus pneumoniae ATCC 49619 at crude extract concentrations of 25%, 50%, 75% and 100% (w/v). Both plants extracts showed strongest activity against S. pneumoniae ATCC 49619 at extract concentration of 75%.   In addition, the extracts of both plants have inhibitory activity against growth of the clinical isolate Streptococcus pneumoniae PU 067. Both plant extracts showed strongest activity against S. pneumoniae PU 067 at extract concentration of 100%.  Therefore, leaf extracts of Anredera cordifolia (Ten.) Steenis and Muntingia calabura L. can potentially be used as a source of antibacterial agent for Streptococcus pneumoniae. Keywords: Antibacterial agent, Anredera cordifolia (Ten.) Steenis, Muntingia calabura L., Streptococcus pneumoniae.

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