Patent Evaluation Anti-infectives: Glycopeptide antibiotic derivatives active against Vancomycin-resistant Gram-positive bacteria

1996 ◽  
Vol 6 (1) ◽  
pp. 73-75
Keyword(s):  
Glycopeptide Antibiotic ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Patent Evaluation ◽  
Vancomycin Resistant

scholarly journals In Vitro and In Vivo Activities of DA-7867, a New Oxazolidinone, against Aerobic Gram-Positive Bacteria

2005 ◽  
Vol 49 (6) ◽  
pp. 2498-2500 ◽  
Author(s):  
Eun Jeong Yoon ◽  
Yeong Woo Jo ◽  
Sung Hak Choi ◽  
Tae Ho Lee ◽  
Jae Keol Rhee ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Streptococcus Pneumoniae ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Infection Models ◽  
Vancomycin Resistant

ABSTRACT In vitro and in vivo activities of DA-7867 were assessed against methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, and penicillin-resistant Streptococcus pneumoniae. All isolates were inhibited by DA-7867 at ≤0.78 μg/ml, a four-times-lower concentration than that of inhibition by linezolid. For murine infection models, DA-7867 also exhibited greater efficacy than linezolid against all isolates tested.

scholarly journals Activities of Oxadiazole Antibacterials against Staphylococcus aureus and Other Gram-Positive Bacteria

2018 ◽  
Vol 62 (8) ◽  
Author(s):  
Sara Ceballos ◽  
Choon Kim ◽  
Derong Ding ◽  
Shahriar Mobashery ◽  
Mayland Chang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Content Type ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant ◽  
Mrsa Strains

ABSTRACT The activities of four oxadiazoles were investigated with 210 methicillin-resistant Staphylococcus aureus (MRSA) strains. MIC50 and MIC90 values of 1 to 2 and 4 μg/ml, respectively, were observed. We also evaluated the activity of oxadiazole ND-421 against other staphylococci and enterococci and in the presence of oxacillin for selected MRSA strains. The MIC for ND-421 is lowered severalfold in combination with oxacillin, as they synergize. The MIC90 of ND-421 against vancomycin-resistant enterococci is ≤1 μg/ml.

scholarly journals Resistance of Gram-Positive Bacteria to Current Antibacterial Agents and Overcoming Approaches

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2888 ◽  
Author(s):  
Buthaina Jubeh ◽  
Zeinab Breijyeh ◽  
Rafik Karaman
Keyword(s):  
Turning Point ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Gram Positive ◽  
Medical Interventions ◽  
Gram Positive Bacteria ◽  
New Antibiotics ◽  
Vancomycin Resistant ◽  
New Treatments ◽  
Emergence Of Resistance

The discovery of antibiotics has created a turning point in medical interventions to pathogenic infections, but unfortunately, each discovery was consistently followed by the emergence of resistance. The rise of multidrug-resistant bacteria has generated a great challenge to treat infections caused by bacteria with the available antibiotics. Today, research is active in finding new treatments for multidrug-resistant pathogens. In a step to guide the efforts, the WHO has published a list of the most dangerous bacteria that are resistant to current treatments and requires the development of new antibiotics for combating the resistance. Among the list are various Gram-positive bacteria that are responsible for serious healthcare and community-associated infections. Methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and drug-resistant Streptococcus pneumoniae are of particular concern. The resistance of bacteria is an evolving phenomenon that arises from genetic mutations and/or acquired genomes. Thus, antimicrobial resistance demands continuous efforts to create strategies to combat this problem and optimize the use of antibiotics. This article aims to provide a review of the most critical resistant Gram-positive bacterial pathogens, their mechanisms of resistance, and the new treatments and approaches reported to circumvent this problem.

scholarly journals Comparative Surveillance Study of Telavancin Activity against Recently Collected Gram-Positive Clinical Isolates from across the United States

2008 ◽  
Vol 52 (7) ◽  
pp. 2383-2388 ◽  
Author(s):  
Deborah C. Draghi ◽  
Bret M. Benton ◽  
Kevin M. Krause ◽  
Clyde Thornsberry ◽  
Chris Pillar ◽  
...  
Keyword(s):  
United States ◽  
The United States ◽  
Clinical Isolates ◽  
Surveillance Study ◽  
Coagulase Negative Staphylococci ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Serious Infections ◽  
Wide Range ◽  
Vancomycin Resistant

ABSTRACT Telavancin is an investigational, rapidly bactericidal lipoglycopeptide antibiotic that is being developed to treat serious infections caused by gram-positive bacteria. A baseline prospective surveillance study was conducted to assess telavancin activity, in comparison with other agents, against contemporary clinical isolates collected from 2004 to 2005 from across the United States. Nearly 4,000 isolates were collected, including staphylococci, enterococci, and streptococci (pneumococci, beta-hemolytic, and viridans). Telavancin had potent activity against Staphylococcus aureus and coagulase-negative staphylococci (MIC range, 0.03 to 1.0 μg/ml), independent of resistance to methicillin or to multiple agents. Telavancin activity was particularly potent against all streptococcal groups (MIC90s, 0.03 to 0.12 μg/ml). Telavancin had excellent activity against vancomycin-susceptible enterococci (MIC90, 1 μg/ml) and was active against VanB strains of vancomycin-resistant enterococci (MIC90, 2 μg/ml) but less active against VanA strains (MIC90, 8 to 16 μg/ml). Telavancin also demonstrated activity against vancomycin-intermediate S. aureus and vancomycin-resistant S. aureus strains (MICs, 0.5 μg/ml to 1.0 μg/ml and 1.0 μg/ml to 4.0 μg/ml, respectively). These data may support the efficacy of telavancin for treatment of serious infections with a wide range of gram-positive organisms.

scholarly journals Linezolid induced thrombocytopenia

2020 ◽  
Vol 9 (7) ◽  
pp. 1130
Author(s):  
P. Muthamil
Keyword(s):  
Platelet Count ◽  
Renal Transplantation ◽  
Antibiotic Prophylaxis ◽  
Rare Case ◽  
Gram Positive ◽  
Platelet Counts ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant

Linezolid, an oxazolidinone antibiotic active against gram-positive bacteria is used in the treatment of vancomycin resistant Enterococci and MRSA. It is generally tolerated except for the 32% chance of thrombocytopenia on long term usage of linezolid. A 25-year-old male after renal transplantation was administered linezolid for antibiotic prophylaxis. His platelet count dropped from 1,68,000 cells to 74,000 on day 2. The platelet counts further dropped to 58,000 on day 3, followed which linezolid was withdrawn. His platelet improved to 88,000 on day 5 following withdrawal of linezolid. Though we are vigilant about thrombocytopenia on long term usage of linezolid, here we report a rare case of linezolid induced thrombocytopenia within 2 days of starting the antibiotic. This necessitates the increased vigilance on linezolid usage. Platelet count needs to be monitored as early as the start of treatment with linezolid.

Antimicrobial-Resistant Gram-Positive Bacteria in PD Peritonitis and the Newer Antibiotics Used to Treat Them

2005 ◽  
Vol 25 (4) ◽  
pp. 313-319 ◽  
Author(s):  
William Salzer
Keyword(s):  
Methicillin Resistant Staphylococcus Aureus ◽  
Natural Habitat ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
The Past ◽  
Vancomycin Resistant Enterococci ◽  
Resistant Strains ◽  
Vancomycin Resistant ◽  
Novel Antibiotics

The incidence of resistant gram-positive bacteria in nosocomial and, more recently, community-acquired infections is increasing. Staphylococci, because of their natural habitat on the skin, have always been the leading cause of peritonitis in patients receiving peritoneal dialysis (PD). These organisms have demonstrated a remarkable ability to develop resistance to antibiotics, first with penicillin, then antistaphylococcal penicillins (methicillin-resistant Staphylococcus aureus), and more recently, strains expressing resistance to vancomycin (vancomycin-intermediate and vancomycin-resistant S. aureus) have emerged. Enterococci are normal inhabitants of the gastrointestinal tract and occasionally cause PD peritonitis. In the past 15 years, vancomycin-resistant enterococci have emerged as significant pathogens in many areas. In the past 5 years, novel antibiotics that have activity on gram-positive bacteria, including vancomycin-resistant strains, have become available. The problem of resistant gram-positive bacteria in PD peritonitis, their therapy, and the role of these newer agents, quinupristin/dalfopristin, linezolid, and daptomycin, are reviewed.

Vancomycin in Pediatrics

1983 ◽  
Vol 5 (6) ◽  
pp. 185-189
Author(s):  
Mark D. Greenfield ◽  
Arnold L. Smith
Keyword(s):  
Renal Failure ◽  
Antibacterial Activity ◽  
Pseudomembranous Colitis ◽  
Glycopeptide Antibiotic ◽  
Gram Positive ◽  
Adverse Side Effects ◽  
Gram Positive Bacteria ◽  
Serious Infections ◽  
Wide Range ◽  
Anephric Patients

Vancomycin, a complex glycopeptide antibiotic, has achieved somewhat limited use since its introduction in 1956. It has excellent antibacterial activity against a variety of Gram-positive organisms, including those resistant to semisynthetic penicillins such as methicillin. Because of its higher potential for adverse side effects, such as thrombophlebitis and ototoxicity, it should be reserved for illnesses associated with methicillin-resistant staphylococci or in patients who have serious allergies to the penicillins. It has shown excellent effectiveness in a wide range of serious infections due to Gram-positive bacteria. Vancomycin should be administered intravenously, except in the case of staphylococcal or pseudomembranous colitis associated with C difficile in which oral administration is the appropriate route. In infections with enterococci, combination with an aminoglycoside is indicated as synergism occurs. It is excreted by the kidney; extra care must be taken in treating patients with renal failure. Dosing in anephric patients undergoing dialysis is greatly simplified by its prolonged half-life and is usually necessary only every seven to 14 days. Monitoring the serum concentration is desirable in all patients receiving vancomycin to ensure an efficacious, but nontoxic level.

Redox-active cationic organoiron complex: a promising lead structure for developing antimicrobial agents with activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium

RSC Advances ◽  
2015 ◽  
Vol 5 (105) ◽  
pp. 86421-86427 ◽  
Author(s):  
Alaa S. Abd-El-Aziz ◽  
Christian Agatemor ◽  
Nola Etkin ◽  
David P. Overy ◽  
Russell G. Kerr
Keyword(s):  
Antimicrobial Agents ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Multidrug Resistant ◽  
Gram Positive ◽  
Lead Structure ◽  
Gram Positive Bacteria ◽  
Redox Active ◽  
Vancomycin Resistant ◽  
Organoiron Complexes ◽  
Multidrug Resistant Strain

A redox-active, cationic organoiron complexes active against multidrug-resistant strain of Gram-positive bacteria is presented as a potential new lead structure for the design of antimicrobial agents.

Teicoplanin: A New Glycopeptide Antibiotic Complex

1988 ◽  
Vol 22 (3) ◽  
pp. 218-226 ◽  
Author(s):  
Najib Babul ◽  
Mary Pasko
Keyword(s):  
Glycopeptide Antibiotic ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Elimination Half ◽  
Serum Aminotransferases ◽  
Transient Elevation ◽  
Aerobic And Anaerobic ◽  
Efficacy Profile

The chemistry, microbiology, pharmacokinetics, clinical efficacy, and adverse effect profile of teicoplanin are reviewed and, where appropriate, compared with vancomycin. Teicoplanin is a glycopeptide antibiotic with potent bactericidal activity against a wide variety of aerobic and anaerobic gram-positive bacteria. In contrast to the structurally related vancomycin, teicoplanin has a prolonged elimination half-life of approximately 60 hours and it may be safely administered by the intramuscular route. Adverse effects of teicoplanin include ototoxicity, nephrotoxicity, skin rash, eosinophilia, neutropenia, and transient elevation of serum aminotransferases. Teicoplanin may be beneficial as an alternative to vancomycin for patients with poor vascular access and in those requiring long-term outpatient therapy. The role of teicoplanin in the treatment and prophylaxis of gram-positive infections will ultimately depend on its unfolding safety and efficacy profile.

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