oxazolidinones

Summary

Summary: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.

Top Publications

  1. pmc Two novel point mutations in clinical Staphylococcus aureus reduce linezolid susceptibility and switch on the stringent response to promote persistent infection
    Wei Gao
    Department of Microbiology, Monash University, Clayton, Victoria, Australia
    PLoS Pathog 6:e1000944. 2010
  2. pmc The Cfr rRNA methyltransferase confers resistance to Phenicols, Lincosamides, Oxazolidinones, Pleuromutilins, and Streptogramin A antibiotics
    Katherine S Long
    Institute of Molecular Biology and Physiology, University of Copenhagen, Sølvgade 83 H, DK 1307 Copenhagen K, Denmark
    Antimicrob Agents Chemother 50:2500-5. 2006
  3. ncbi Assessment of linezolid resistance mechanisms among Staphylococcus epidermidis causing bacteraemia in Rome, Italy
    Rodrigo E Mendes
    JMI Laboratories, North Liberty, IA 52317, USA
    J Antimicrob Chemother 65:2329-35. 2010
  4. ncbi Oxazolidinones: activity, mode of action, and mechanism of resistance
    Bulent Bozdogan
    Department of Pathology, Penn State University Hershey Medical Center, H083, 500 University Drive, PO Box 850 Hershey, PA 17033, USA
    Int J Antimicrob Agents 23:113-9. 2004
  5. ncbi The oxazolidinones: past, present, and future
    Karen Joy Shaw
    Trius Therapeutics, Inc, Department of Biology, San Diego, California 92121, USA
    Ann N Y Acad Sci 1241:48-70. 2011
  6. pmc Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport
    Eric J Niesor
    Pharmaceuticals Division, F Hoffmann La Roche Ltd, Basel, Switzerland
    J Lipid Res 51:3443-54. 2010
  7. pmc Acquisition of a natural resistance gene renders a clinical strain of methicillin-resistant Staphylococcus aureus resistant to the synthetic antibiotic linezolid
    Seok Ming Toh
    Center for Pharmaceutical Biotechnology, University of Illinois, Chicago, IL 60607, USA
    Mol Microbiol 64:1506-14. 2007
  8. pmc Activities of clindamycin, daptomycin, doxycycline, linezolid, trimethoprim-sulfamethoxazole, and vancomycin against community-associated methicillin-resistant Staphylococcus aureus with inducible clindamycin resistance in murine thigh infection and in vi
    Kerry L LaPlante
    Anti Infective Research Laboratory, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, Michigan 48201, USA
    Antimicrob Agents Chemother 52:2156-62. 2008
  9. ncbi Linezolid, the first oxazolidinone antibacterial agent
    Karen L Leach
    Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Ann N Y Acad Sci 1222:49-54. 2011
  10. ncbi Virulence factor expression by Gram-positive cocci exposed to subinhibitory concentrations of linezolid
    Curtis G Gemmell
    University Department of Bacteriology and Immunology, University of Glasgow, Royal Infirmary, 84 86 Castle Street, Glasgow G4 OSF, UK
    J Antimicrob Chemother 50:665-72. 2002

Detail Information

Publications278 found, 100 shown here

  1. pmc Two novel point mutations in clinical Staphylococcus aureus reduce linezolid susceptibility and switch on the stringent response to promote persistent infection
    Wei Gao
    Department of Microbiology, Monash University, Clayton, Victoria, Australia
    PLoS Pathog 6:e1000944. 2010
    ..These results reinforce the exquisite adaptability of S. aureus and show how subtle molecular changes cause major alterations in bacterial behaviour, as well as highlighting potential weaknesses of current antibiotic treatment regimens...
  2. pmc The Cfr rRNA methyltransferase confers resistance to Phenicols, Lincosamides, Oxazolidinones, Pleuromutilins, and Streptogramin A antibiotics
    Katherine S Long
    Institute of Molecular Biology and Physiology, University of Copenhagen, Sølvgade 83 H, DK 1307 Copenhagen K, Denmark
    Antimicrob Agents Chemother 50:2500-5. 2006
    ..The phenotype is named PhLOPSA for resistance to the following drug classes: Phenicols, Lincosamides, Oxazolidinones, Pleuromutilins, and Streptogramin A antibiotics...
  3. ncbi Assessment of linezolid resistance mechanisms among Staphylococcus epidermidis causing bacteraemia in Rome, Italy
    Rodrigo E Mendes
    JMI Laboratories, North Liberty, IA 52317, USA
    J Antimicrob Chemother 65:2329-35. 2010
    ..Isolates also showed elevated MICs of macrolide, lincosamide and streptogramin (MLS) compounds, which were investigated...
  4. ncbi Oxazolidinones: activity, mode of action, and mechanism of resistance
    Bulent Bozdogan
    Department of Pathology, Penn State University Hershey Medical Center, H083, 500 University Drive, PO Box 850 Hershey, PA 17033, USA
    Int J Antimicrob Agents 23:113-9. 2004
    b>Oxazolidinones are a new group of antibiotics...
  5. ncbi The oxazolidinones: past, present, and future
    Karen Joy Shaw
    Trius Therapeutics, Inc, Department of Biology, San Diego, California 92121, USA
    Ann N Y Acad Sci 1241:48-70. 2011
    ..Over a dozen oxazolidinones have reached the clinic, but many were discontinued due to lack of differentiated potency, inadequate ..
  6. pmc Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport
    Eric J Niesor
    Pharmaceuticals Division, F Hoffmann La Roche Ltd, Basel, Switzerland
    J Lipid Res 51:3443-54. 2010
    ..These data suggest that modulation of CETP activity by dalcetrapib does not inhibit CETP-induced pre-β-HDL formation, which may be required to increase reverse cholesterol transport...
  7. pmc Acquisition of a natural resistance gene renders a clinical strain of methicillin-resistant Staphylococcus aureus resistant to the synthetic antibiotic linezolid
    Seok Ming Toh
    Center for Pharmaceutical Biotechnology, University of Illinois, Chicago, IL 60607, USA
    Mol Microbiol 64:1506-14. 2007
    ..This is the first example of clinical resistance to the synthetic drug linezolid which involves a natural resistance gene with the capability of disseminating among Gram-positive pathogenic strains...
  8. pmc Activities of clindamycin, daptomycin, doxycycline, linezolid, trimethoprim-sulfamethoxazole, and vancomycin against community-associated methicillin-resistant Staphylococcus aureus with inducible clindamycin resistance in murine thigh infection and in vi
    Kerry L LaPlante
    Anti Infective Research Laboratory, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, Michigan 48201, USA
    Antimicrob Agents Chemother 52:2156-62. 2008
    ..At present, there are several alternatives that appear promising for treating clindamycin resistance-inducible strains of CA-MRSA...
  9. ncbi Linezolid, the first oxazolidinone antibacterial agent
    Karen L Leach
    Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Ann N Y Acad Sci 1222:49-54. 2011
    ....
  10. ncbi Virulence factor expression by Gram-positive cocci exposed to subinhibitory concentrations of linezolid
    Curtis G Gemmell
    University Department of Bacteriology and Immunology, University of Glasgow, Royal Infirmary, 84 86 Castle Street, Glasgow G4 OSF, UK
    J Antimicrob Chemother 50:665-72. 2002
    ..8% bacteria ingested versus 37.5%; P <or= 0.05). A reduction in virulence factor expression at sub-MIC linezolid concentrations may be of benefit in the treatment of Gram-positive infections...
  11. pmc Transferable multidrug resistance plasmid carrying cfr associated with tet(L), ant(4')-Ia, and dfrK genes from a clinical methicillin-resistant Staphylococcus aureus ST125 strain
    Enrique Ruiz de Gopegui
    Servicio de Microbiologia, Hospital Universitari Son Espases, Palma de Mallorca, Spain
    Antimicrob Agents Chemother 56:2139-42. 2012
    ..pERGB was transferable by conjugation and carried the resistance genes cfr (oxazolidinones, phenicols, lincosamides, pleuromutilins, and streptogramin A), ant(4')-Ia (tobramycin), tet(L) (tetracycline),..
  12. ncbi Resistance to linezolid is mediated by the cfr gene in the first report of an outbreak of linezolid-resistant Staphylococcus aureus
    Gracia Morales
    Clinical Microbiology Service, Hospital Clinico San Carlos, Madrid, Spain
    Clin Infect Dis 50:821-5. 2010
    ..We investigated the mechanism of resistance--point mutations in domain V of 23S ribosomal RNA (rRNA) or presence of the cfr gene--involved in the outbreak...
  13. ncbi Linezolid-resistant clinical isolates of meticillin-resistant coagulase-negative staphylococci and Enterococcus faecium from China
    Jia Chang Cai
    2nd Affiliated Hospital of Zhejiang University, Zhejiang University, 88 Jiefang Road, Hangzhou 310009, PR China
    J Med Microbiol 61:1568-73. 2012
    ..There was a clonal dissemination of linezolid-resistant MRCoNS in intensive care units of our hospital, and this is the first report, to our knowledge, of linezolid-resistant staphylococci and enterococci in China...
  14. pmc Hematologic effects of linezolid: summary of clinical experience
    Stanton L Gerson
    Division of Hematology Oncology and Ireland Cancer Center, Case Western Reserve University, University Hospitals of Cleveland, 10900 Euclid Avenue, Cleveland, OH 44106 4937, USA
    Antimicrob Agents Chemother 46:2723-6. 2002
    ..Hematologic abnormalities were consistent with mild, reversible, duration-dependent myelosuppression. Appropriate monitoring is warranted with linezolid use...
  15. pmc Linezolid vs glycopeptide antibiotics for the treatment of suspected methicillin-resistant Staphylococcus aureus nosocomial pneumonia: a meta-analysis of randomized controlled trials
    Allan J Walkey
    Boston University School of Medicine, The Pulmonary Center, 715 Albany St, R 304, Boston, MA 02118, USA
    Chest 139:1148-55. 2011
    ..Societal guidelines suggest linezolid may be the preferred treatment of MRSA nosocomial pneumonia. We investigated the efficacy of linezolid compared with glycopeptide antibiotics (vancomycin or teicoplanin) for nosocomial pneumonia...
  16. ncbi Cost-effectiveness of linezolid and vancomycin in the treatment of surgical site infections
    Asad E Patanwala
    The University of Arizona College of Pharmacy, Tucson, AZ, USA
    Curr Med Res Opin 23:185-93. 2007
    ....
  17. pmc Frovatriptan versus zolmitriptan for the acute treatment of migraine: a double-blind, randomized, multicenter, Italian study
    Vincenzo Tullo
    Department of Clinical Neurosciences, National Neurological Institute Carlo Besta, Via Celoria 11, 20133, Milan, Italy
    Neurol Sci 31:S51-4. 2010
    ..Drug-related adverse events were significantly (p < 0.05) less under F (3 vs. 10). In conclusion, our study suggests that F has a similar efficacy of Z, with some advantage as regards tolerability and recurrence...
  18. pmc Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin
    Jeffrey B Locke
    Trius Therapeutics, Inc, San Diego, CA 92121, USA
    Antimicrob Agents Chemother 53:5275-8. 2009
    ..The oxazolidinone torezolid maintained a >or=8-fold potency advantage over linezolid for both strains...
  19. pmc Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis
    Robert S Wallis
    Pfizer, Groton New London, CT 06320, USA
    Antimicrob Agents Chemother 55:567-74. 2011
    ..06 log) (P = 0.002). In conclusion, PNU-100480 was safe and well tolerated at all tested doses. Further studies in patients with tuberculosis are warranted. Biomarkers can accelerate early development of new tuberculosis treatments...
  20. pmc Novel ribosomal mutations in Staphylococcus aureus strains identified through selection with the oxazolidinones linezolid and torezolid (TR-700)
    Jeffrey B Locke
    Trius Therapeutics, Inc, San Diego, CA 92121, USA
    Antimicrob Agents Chemother 53:5265-74. 2009
    ..These data bring to light a variety of novel and less-characterized mutations associated with S. aureus resistance to oxazolidinones and demonstrate the low resistance potential of torezolid.
  21. pmc Subinhibitory concentrations of linezolid reduce Staphylococcus aureus virulence factor expression
    Katussevani Bernardo
    Institute for Medical Microbiology, Immunology, and Hygiene, Medical Center, University of Cologne, Cologne, Germany
    Antimicrob Agents Chemother 48:546-55. 2004
    ..aureus is especially sensitive to the inhibition of protein synthesis by linezolid, which should be an advantage in the treatment of infections with toxin-producing S. aureus...
  22. ncbi Update on macrolide-lincosamide-streptogramin, ketolide, and oxazolidinone resistance genes
    Marilyn C Roberts
    Department of Environmental and Occupational Health Sciences, School of Public Health and Community Medicine, University of Washington, Seattle, WA, USA
    FEMS Microbiol Lett 282:147-59. 2008
    ..These mobile elements may play a role in the continued spread of the MLSKO resistance genes into new species, genera, and ecosystems...
  23. ncbi Clinical outbreak of linezolid-resistant Staphylococcus aureus in an intensive care unit
    Miguel Sanchez Garcia
    Intensive Care Department, Hospital Clínico San Carlos and Universidad Complutense, 28040 Madrid, Spain
    JAMA 303:2260-4. 2010
    ..Linezolid resistance is extremely uncommon in Staphylococcus aureus...
  24. ncbi Safety of anacetrapib in patients with or at high risk for coronary heart disease
    Christopher P Cannon
    TIMI Study Group, Cardiovascular Division, Brigham and Women s Hospital, Boston, MA 02115, USA
    N Engl J Med 363:2406-15. 2010
    ..Anacetrapib is a cholesteryl ester transfer protein inhibitor that raises high-density lipoprotein (HDL) cholesterol and reduces low-density lipoprotein (LDL) cholesterol...
  25. pmc Genome sequencing of linezolid-resistant Streptococcus pneumoniae mutants reveals novel mechanisms of resistance
    Jie Feng
    Centre de Recherche en Infectiologie, Quebec G1V 4G2, Canada
    Genome Res 19:1214-23. 2009
    ..Whole-genome sequencing and comparative analyses of S. pneumoniae resistant isolates was useful for discovering novel resistance mutations...
  26. ncbi Linezolid for the treatment of infections caused by Gram-positive pathogens in China
    Dong Fang Lin
    Institute of Antibiotics, Huashan Hospital, Fudan University, 12 Wulumuqi Zhong Road, Shanghai 200040, China
    Int J Antimicrob Agents 32:241-9. 2008
    ..3%) vancomycin-treated patients discontinued the study drug because of an AE. Linezolid was well tolerated and effective for the treatment of infections caused by Gram-positive pathogens, including meticillin-resistant S. aureus...
  27. ncbi Novel biaryl oxazolidinones: in vitro and in vivo activities with pharmacokinetics in an animal model
    Tarani Kanta Barman
    Department of Infectious Diseases, New Drug Discovery Research, Ranbaxy Research Laboratories, Gurgaon, Haryana, India
    Int J Antimicrob Agents 33:280-4. 2009
    RBx 1000075 and RBx 1000276, the new investigational oxazolidinones, have an extended spectrum of in vitro activity against Gram-positive pathogens and showed minimum inhibitory concentrations (MICs) lower than comparator drugs...
  28. ncbi Cytokines in periradicular lesions: the effect of linezolid treatment
    John Danin
    Department of Cariology and Endodontics, Karolinska Institutet, Huddinge University Hospital, Sweden
    Oral Surg Oral Med Oral Pathol Oral Radiol Endod 96:492-8. 2003
    ....
  29. pmc In vitro bactericidal activities of linezolid in combination with vancomycin, gentamicin, ciprofloxacin, fusidic acid, and rifampin against Staphylococcus aureus
    Patrick Grohs
    Hopital Europeen Georges Pompidou, Paris, France
    Antimicrob Agents Chemother 47:418-20. 2003
    ..While the combination with linezolid may reduce the emergence of mutants resistant to the associated drugs, the absence of synergy, especially in the case of vancomycin and ciprofloxacin, does not argue in favor of such combinations...
  30. pmc Absolute bioavailability and pharmacokinetics of linezolid in hospitalized patients given enteral feedings
    Paul Beringer
    School of Pharmacy, University of Southern California, Los Angeles, CA 90033, USA
    Antimicrob Agents Chemother 49:3676-81. 2005
    ..Compartmental pharmacokinetic analysis offers a more flexible study application, since bioavailability (F) can be estimated directly with intermixed intravenous/oral doses without a need for a washout period...
  31. ncbi Molecular and epidemiologic characteristics of linezolid-resistant coagulase-negative staphylococci at a tertiary care hospital
    Klaudia Kosowska-Shick
    Department of Pathology, Penn State Hershey Medical Center, Hershey, PA 17033, USA
    Diagn Microbiol Infect Dis 68:34-9. 2010
    ..The increase in linezolid-resistant coagulase-negative staphylococci correlated with nosocomial transmission of selected mutated strains in patients who had received linezolid...
  32. pmc In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens
    Laura Lawrence
    Rib X Pharmaceuticals, Inc, 300 George Street, New Haven, Connecticut 06511, USA
    Antimicrob Agents Chemother 52:1653-62. 2008
    Rx-01_423 and Rx-01_667 are two members of the family of oxazolidinones that were designed using a combination of computational and medicinal chemistry and conventional biological techniques...
  33. pmc Characterization of methicillin-resistant Staphylococcus aureus strains recovered from a phase IV clinical trial for linezolid versus vancomycin for treatment of nosocomial pneumonia
    Rodrigo E Mendes
    JMI Laboratories, North Liberty, Iowa, USA
    J Clin Microbiol 50:3694-702. 2012
    ..The USA300 rate corroborates previous reports describing increased prevalence of USA300 strains causing invasive infections. The prevalence of hVISA was elevated in Asia, and these strains were associated with CC5...
  34. ncbi Linezolid absolute bioavailability and the effect of food on oral bioavailability
    I R Welshman
    Department of Clinical Pharmacology, Pharmacia, 301 Henrietta St, Kalamazoo, MI 49007, USA
    Biopharm Drug Dispos 22:91-7. 2001
    ..As expected, C(max) was statistically different between the two treatments. However, the mean absolute bioavailability (F) of the tablet, using the IV sterile solution as the reference treatment, was 103% (+/-20%)...
  35. pmc Comparative in vivo efficacies of epithelial lining fluid exposures of tedizolid, linezolid, and vancomycin for methicillin-resistant Staphylococcus aureus in a mouse pneumonia model
    Pamela R Tessier
    Center for Anti Infective Research and Development, Hartford Hospital, Hartford, Connecticut, USA
    Antimicrob Agents Chemother 56:2342-6. 2012
    ..TZD and linezolid showed similar efficacies in this MRSA pneumonia model...
  36. ncbi The role of diabetes mellitus in the treatment of skin and skin structure infections caused by methicillin-resistant Staphylococcus aureus: results from three randomized controlled trials
    Benjamin A Lipsky
    Medical Service, VA Puget Sound Health Care System, 1880 S Columbian Way S 111 GIMC, Seattle, WA 98108 1587, USA
    Int J Infect Dis 15:e140-6. 2011
    ..To compare outcomes of treating complicated skin and skin structure infections (cSSSI) caused by methicillin-resistant Staphylococcus aureus (MRSA) with linezolid versus vancomycin in diabetic and non-diabetic patients...
  37. ncbi In vitro susceptibility of Gram-positive pathogens to linezolid and teicoplanin and effect on outcome in critically ill patients
    A Peter R Wilson
    Department of Clinical Microbiology, University College London Hospitals, 46 Cleveland Street, London W1T 4JF, UK
    J Antimicrob Chemother 58:470-3. 2006
    ..To determine the prevalence of teicoplanin and linezolid resistance amongst Gram-positive pathogens isolated in the intensive care unit (ICU) and the impact of any resistance on clinical outcome...
  38. ncbi Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib
    Cameron J Smith
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, United States
    J Med Chem 54:4880-95. 2011
    ....
  39. pmc Changes in lipoprotein subfraction concentration and composition in healthy individuals treated with the CETP inhibitor anacetrapib
    Ronald M Krauss
    Children s Hospital Oakland Research Institute, Oakland, CA, USA
    J Lipid Res 53:540-7. 2012
    ..The impact of these changes on cardiovascular risk remains to be determined...
  40. ncbi Linezolid pharmacokinetics and pharmacodynamics in clinical treatment
    Matthew S Dryden
    Department of Microbiology, Royal Hampshire County Hospital, Romsey Road, Winchester, UK
    J Antimicrob Chemother 66:iv7-iv15. 2011
    ....
  41. ncbi Pharmacokinetics, metabolism, and excretion of linezolid following an oral dose of [(14)C]linezolid to healthy human subjects
    J G Slatter
    Global Metabolism and Investigative Sciences, Pharmacia Corporation, 301 Henrietta St, Kalamazoo, MI 49007, USA
    Drug Metab Dispos 29:1136-45. 2001
    Linezolid (Zyvox), the first of a new class of antibiotics, the oxazolidinones, is approved for treatment of Gram-positive bacterial infections, including resistant strains...
  42. ncbi Linezolid: pharmacokinetic and pharmacodynamic evaluation of coadministration with pseudoephedrine HCl, phenylpropanolamine HCl, and dextromethorpan HBr
    P E Hendershot
    Clinical Pharmacology, Pharmacia and Upjohn, Kalamazoo, Michigan 49007-4940, USA
    J Clin Pharmacol 41:563-72. 2001
    ..No restrictions are indicated for the coadministration of dextromethorphan and linezolid...
  43. pmc Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects
    Rajesh Krishna
    Merck and Co, Inc, Whitehouse Station, NJ 07065 0900, USA
    Br J Clin Pharmacol 68:535-45. 2009
    ....
  44. pmc Serum and cerebrospinal fluid concentrations of linezolid in neurosurgical patients
    Pavlos Myrianthefs
    Athens University School of Nursing ICU, Athens, Greece
    Antimicrob Agents Chemother 50:3971-6. 2006
    ..These findings suggest that linezolid may achieve adequate concentrations in the CSF of patients requiring antibiotics for the management or prophylaxis of CNS infections caused by gram-positive pathogens...
  45. pmc Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects
    Rajesh Krishna
    Merck and Co, Inc, Whitehouse Station, NJ, USA
    Br J Clin Pharmacol 67:520-6. 2009
    ..Because of the likely use of anacetrapib with hydroxy-3-methylglutaryl coenzyme A reductase inhibitors, we aimed to evaluate the potential for a pharmacokinetic interaction with simvastatin...
  46. ncbi Complicated skin and skin-structure infections and catheter-related bloodstream infections: noninferiority of linezolid in a phase 3 study
    Mark H Wilcox
    Department of Microbiology, Leeds General Infirmary and University of Leeds Teaching Hospitals, Leeds, England
    Clin Infect Dis 48:203-12. 2009
    ..Catheter-related bloodstream infection (CRBSI) causes substantial morbidity and mortality, but few randomized, controlled studies have been conducted to guide therapeutic interventions...
  47. ncbi Addition of PNU-100480 to first-line drugs shortens the time needed to cure murine tuberculosis
    Kathy N Williams
    Center for Tuberculosis Research, Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland 21231, USA
    Am J Respir Crit Care Med 180:371-6. 2009
    ..We recently reported strong bactericidal activity of the oxazolidinone PNU-100480 and its ability to increase the initial bactericidal effect of various combinations of first-line tuberculosis drugs and moxifloxacin in a murine model...
  48. ncbi Different effects of compounds decreasing cholesteryl ester transfer protein activity on lipoprotein metabolism
    Eric J Niesor
    Pharmaceuticals Division, F Hoffmann La Roche Ltd, Basel, Switzerland
    Curr Opin Lipidol 22:288-95. 2011
    ....
  49. ncbi Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction
    D E Gutstein
    Merck Sharp and Dohme Corp, Rahway, New Jersey, USA
    Clin Pharmacol Ther 91:109-22. 2012
    ..We also describe strategies to target HDL-C, discuss the mechanism underlying CETP inhibition and its effects on lipid biology, and give an overview of other CETP inhibitors that are currently in development...
  50. ncbi Anacetrapib: hope for CETP inhibitors?
    Ronen Gurfinkel
    Robarts Research Institute and Schulich School of Medicine and Dentistry, University of Western Ontario, London, Ontario, Canada, N6A 5K8
    Cardiovasc Ther 29:327-39. 2011
    ..This article will briefly review the HDL-C raising through CETP inhibition as an antiatherogenic strategy with a specific focus on anacetrapib...
  51. ncbi Comparison of serotonin toxicity with concomitant use of either linezolid or comparators and serotonergic agents: an analysis of Phase III and IV randomized clinical trial data
    Jill M Butterfield
    Pharmacy Practice, Albany College of Pharmacy and Health Sciences, Albany, NY, USA
    J Antimicrob Chemother 67:494-502. 2012
    ..All reported adverse events were evaluated for serotonin toxicity using exact and surrogate terms consistent with Sternbach Criteria and Hunter Serotonin Toxicity Criteria...
  52. ncbi Linezolid versus vancomycin for treatment of resistant Gram-positive infections in children
    Sheldon L Kaplan
    Baylor College of Medicine and Texas Children s Hospital, 6621 Fannin Street, MC3 2371, Feigin Center No 1150, Houston, TX 77030, USA
    Pediatr Infect Dis J 22:677-86. 2003
    ..Pediatric infections caused by resistant Gram-positive infections are an increasing concern with limited treatment options. Linezolid, a new oxazolidinone, is active against staphylococci, streptococci and enterococci...
  53. ncbi Stability of linezolid activity in an era of mobile oxazolidinone resistance determinants: results from the 2009 Zyvox® Annual Appraisal of Potency and Spectrum program
    Douglas J Biedenbach
    JMI Laboratories, North Liberty, IA 52317, USA
    Diagn Microbiol Infect Dis 68:459-67. 2010
    ..48%) having the mobile cfr gene. The results of this study demonstrate that linezolid continues to be effective in vitro against MDR pathogens, and the resistance rates appear stable...
  54. ncbi Anacetrapib and dalcetrapib: two novel cholesteryl ester transfer protein inhibitors
    Marta A Miyares
    Pharmacy Department, Jackson Memorial Hospital, Miami, FL, USA
    Ann Pharmacother 45:84-94. 2011
    ....
  55. ncbi Vancomycin versus linezolid in the treatment of methicillin-resistant Staphylococcus aureus nosocomial pneumonia: implications of the ZEPHyR trial
    Cesar Alaniz
    University of Michigan Hospitals and College of Pharmacy, Ann Arbor, USA
    Ann Pharmacother 46:1432-5. 2012
    ..Results of the ZEPHyR trial do not support routine use of linezolid for the treatment of MRSA pneumonia...
  56. ncbi Use of pyrosequencing to identify point mutations in domain V of 23S rRNA genes of linezolid-resistant Staphylococcus aureus and Staphylococcus epidermidis
    W Zhu
    Division of Healthcare Quality Promotion, Centers for Disease Control and Prevention, 1600 Clifton Road, MS G08, Atlanta, GA 30333, USA
    Eur J Clin Microbiol Infect Dis 26:161-5. 2007
    ..epidermidis that were associated with linezolid resistance. A C2534T mutation was identified in S. epidermidis that was not previously reported in a linezolid-resistant isolate...
  57. pmc Rapid detection and estimation by pyrosequencing of 23S rRNA genes with a single nucleotide polymorphism conferring linezolid resistance in Enterococci
    Alistair Sinclair
    Antibiotic Resistance Monitoring and Reference Laboratory, Specialist and Reference Microbiology Division, Health Protection Agency Colindale, London NW9 5HT, United Kingdom
    Antimicrob Agents Chemother 47:3620-2. 2003
    ..A good correlation was found between linezolid MICs and the number of 23S rRNA gene copies carrying the mutation...
  58. ncbi Linezolid compared with teicoplanin for the treatment of suspected or proven Gram-positive infections
    Mark Wilcox
    Department of Microbiology, Leeds General Infirmary and University of Leeds Teaching Hospitals, Old Medical School, Leeds LS1 3EX
    J Antimicrob Chemother 53:335-44. 2004
    ..However, antibiotic discontinuation rates as a result of drug related adverse events were similar (4.7% in the linezolid group versus 3.7%). Linezolid was clinically superior to teicoplanin in the treatment of Gram-positive infections...
  59. ncbi Linezolid in the treatment of methicillin-resistant staphylococcal post-neurosurgical meningitis: a series of 17 cases
    Oguz Resat Sipahi
    Department of Infectious Diseases and Clinical Microbiology, Izmir, Turkey
    Scand J Infect Dis 43:757-64. 2011
    ..The aim of this study was to evaluate the efficacy of linezolid in methicillin-resistant staphylococcal (methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant coagulase-negative Staphylococcus (MRCoNS)) meningitis...
  60. ncbi Treatment of meningitis caused by methicillin-resistant Staphylococcus aureus with linezolid
    A T Kessler
    Department of Medicine, Northside Cherokee Hospital, Atlanta, GA 30013, USA
    Infection 35:271-4. 2007
    ..Clinical trials to address the role of linezolid in CNS infections are urgently needed...
  61. ncbi Linezolid diminishes inflammatory cytokine production from human peripheral blood mononuclear cells
    Pilar Garcia-Roca
    Departamento de Inmunoquímica y Biología Celular, Hospital Infantil de Mexico, Federico Gomez, Mexico, D F, Mexico
    Arch Med Res 37:31-5. 2006
    ..Some antibiotics have been reported to have immunomodulatory effects in addition to their antimicrobial activity. We examined the effect of linezolid on cytokine synthesis...
  62. ncbi Efficacy and tolerability of oral zolmitriptan in menstrually associated migraine: a randomized, prospective, parallel-group, double-blind, placebo-controlled study
    Elizabeth Loder
    Spaulding Rehabilitation Hospital, Boston, Mass 02114, USA
    Headache 44:120-30. 2004
    ..Approximately 60% of female migraineurs report experiencing migraine in association with menstruation, while 7% to 25% experience attacks almost exclusively with menstruation...
  63. pmc LEADER Program results for 2009: an activity and spectrum analysis of linezolid using 6,414 clinical isolates from 56 medical centers in the United States
    David J Farrell
    JMI Laboratories, North Liberty, IA 52317, USA
    Antimicrob Agents Chemother 55:3684-90. 2011
    ..Linezolid continues to exhibit excellent activity and spectrum, and this study documents the need for continued monitoring of emerging mechanisms of resistance over a wide geographic area...
  64. pmc Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3
    Jeffrey B Locke
    Trius Therapeutics, Inc, 6310 Nancy Ridge Drive, Suite 105, San Diego, CA 92121, USA
    Antimicrob Agents Chemother 54:5352-5. 2010
    ..LZD MIC values (16, 32, or 64 μg/ml) correlated with the presence and severity of the L3 mutation. All isolates had TR-700 (torezolid) MIC values of ≤ 2 μg/ml...
  65. ncbi Properties and inhibition of the first two enzymes of the non-mevalonate pathway of isoprenoid biosynthesis
    C Mueller
    Botanical Institute II, University of Karlsruhe, Kaiserstr 12, D 76128 Karlsruhe, Germany
    Biochem Soc Trans 28:792-3. 2000
    ..The DXR of plants, isolated from barley seedlings, shows a pH optimum of 8.1, which is typical for enzymes active in the chloroplast stroma...
  66. pmc Promising antituberculosis activity of the oxazolidinone PNU-100480 relative to that of linezolid in a murine model
    K N Williams
    Department of Medicine, Center for Tuberculosis Research, Johns Hopkins University School of Medicine, Baltimore, MD 21231, USA
    Antimicrob Agents Chemother 53:1314-9. 2009
    ..In this study, we compared the pharmacokinetics and the antituberculosis activities of these two oxazolidinones over a range of doses and found that linezolid has limited activity at clinically relevant doses in the murine ..
  67. pmc Polyphyletic emergence of linezolid-resistant staphylococci in the United States
    Agnes Wong
    Department of Microbiology and Immunology, New York Medical College, Valhalla, NY, USA
    Antimicrob Agents Chemother 54:742-8. 2010
    ..epidermidis isolates. These findings suggest that linezolid resistance has emerged independently in multiple clones of S. aureus and with a variety of ribosomal mutations in multiple clones of S. epidermidis...
  68. pmc Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances
    Silke Besier
    Institut für Medizinische Mikrobiologie und Krankenhaushygiene, Klinikum der Johann Wolfgang Goethe Universitat, Frankfurt am Main, Germany
    Antimicrob Agents Chemother 52:1570-2. 2008
    ....
  69. pmc In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model
    Cedric Jacqueline
    Universite de Nantes, Nantes Atlantique Universites, Therapeutiques Cliniques et Experimentales des Infections, EA3826, UFR Medecine, Nantes, France
    Antimicrob Agents Chemother 51:3397-400. 2007
    ..After a 4-day treatment, ceftaroline exhibited superior bactericidal in vivo activity against resistant S. aureus strains and appeared to be the most effective drug against a heterogeneous glycopeptide-intermediate S. aureus strain...
  70. ncbi Vancomycin MIC creep in non-vancomycin-intermediate Staphylococcus aureus (VISA), vancomycin-susceptible clinical methicillin-resistant S. aureus (MRSA) blood isolates from 2001-05
    Gregory Steinkraus
    New Hanover Regional Medical Center, 2131 South 17th Street, Wilmington, NC 28402, USA
    J Antimicrob Chemother 60:788-94. 2007
    ..Additionally, MIC trends were evaluated for oxacillin, linezolid and daptomycin...
  71. ncbi Linezolid versus vancomycin for the treatment of gram-positive bacterial infections: meta-analysis of randomised controlled trials
    Liang Beibei
    Department of Clinical Pharmacology, General Hospital of Chinese People s Liberation Army, 28 Fuxing Road, Beijing, PR China
    Int J Antimicrob Agents 35:3-12. 2010
    ..There is superior clinical and microbiological outcome with linezolid in complicated skin and soft-tissue infections caused by Staphylococcus aureus...
  72. ncbi Early microbiological response to linezolid vs vancomycin in ventilator-associated pneumonia due to methicillin-resistant Staphylococcus aureus
    Richard G Wunderink
    Division of Pulmonary and Critical Care, Northwestern University Feinberg School of Medicine, Chicago, IL 60611, USA
    Chest 134:1200-7. 2008
    ..This prospective, open-label, multicenter clinical trial compared the early microbiological efficacy of linezolid (LZD) therapy with that of vancomycin (VAN) therapy in patients with MRSA VAP...
  73. ncbi Activity of oxazolidinone TR-700 against linezolid-susceptible and -resistant staphylococci and enterococci
    David M Livermore
    Antibiotic Resistance Monitoring and Reference Laboratory, Health Protection Agency Centre for Infections, 61 Colindale Avenue, London NW95EQ, UK
    J Antimicrob Chemother 63:713-5. 2009
    ..TR-700 is the active moiety of TR-701 (DA-7157), a new oral/intravenous oxazolidinone prodrug. We examined its activity against linezolid-susceptible and -resistant staphylococci and enterococci...
  74. ncbi Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by Nocardia brasiliensis
    Nelly Alejandra Espinoza-González
    Servicio de Dermatologia, Hospital Universitario Dr Jose E Gonzalez, Ave Madero y Gonzalitos S N Col Mitras Centro Monterrey, N L Mexico
    Molecules 13:31-40. 2008
    Two recently synthesized oxazolidinones: (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyloxazolidin-2-one (DA-7157) and its corresponding pro-drug (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-..
  75. ncbi Spread of ampicillin/vancomycin-resistant Enterococcus faecium of the epidemic-virulent clonal complex-17 carrying the genes esp and hyl in German hospitals
    I Klare
    Robert Koch Institute, Wernigerode Branch, Burgstr 37, 38855, Wernigerode, Germany
    Eur J Clin Microbiol Infect Dis 24:815-25. 2005
    ..In conclusion, it is very important to monitor the occurrence of epidemic-virulent clonal complex-17 strains of E. faecium to prevent their spread in hospitals, especially if they are resistant to glycopeptides and linezolid...
  76. ncbi An outbreak of colonization with linezolid-resistant Staphylococcus epidermidis in an intensive therapy unit
    Sinead Kelly
    Department of Clinical Microbiology, The Adelaide and Meath Hospital incorporating the National Children s Hospital, Tallaght, Dublin 24, Ireland
    J Antimicrob Chemother 61:901-7. 2008
    ..To report an outbreak of colonization with linezolid-resistant Staphylococcus epidermidis in an intensive therapy unit (ITU)...
  77. ncbi Antimicrobial resistance to linezolid
    Venkata G Meka
    Division of Infectious Diseases, Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02115, USA
    Clin Infect Dis 39:1010-5. 2004
    ....
  78. ncbi Intracellular accumulation of linezolid in Escherichia coli, Citrobacter freundii and Enterobacter aerogenes: role of enhanced efflux pump activity and inactivation
    Anja Schumacher
    Center for Infectious Diseases and Travel Medicine, University Hospital Hugstetter Strasse 55, Freiburg, Germany
    J Antimicrob Chemother 59:1261-4. 2007
    ..We hypothesized that the poor activity of linezolid in Gram-negative bacteria is in part caused by relatively low intracellular concentration due to efflux...
  79. ncbi Pharmacokinetic studies of linezolid and teicoplanin in the critically ill
    Tony Whitehouse
    Bloomsbury Institute of Intensive Care Medicine, Department of Medicine, University College London, London, UK
    J Antimicrob Chemother 55:333-40. 2005
    ..To determine the pharmacokinetic characteristics of linezolid and teicoplanin in critically ill patients...
  80. ncbi United States resistance surveillance results for linezolid (LEADER Program for 2007)
    Ronald N Jones
    JMI Laboratories, North Liberty, IA 52317, USA Tufts University School of Medicine, Boston, MA 02111, USA
    Diagn Microbiol Infect Dis 62:416-26. 2008
    ..aureus and Staphylococcus epidermidis strains from Arizona and Ohio. The LEADER Program appears to be an effective and sensitive surveillance tool to detect novel resistance phenotypes and genotypes...
  81. ncbi Linezolid versus glycopeptide or beta-lactam for treatment of Gram-positive bacterial infections: meta-analysis of randomised controlled trials
    Matthew E Falagas
    Alfa Institute of Biomedical Sciences, Athens, Greece
    Lancet Infect Dis 8:53-66. 2008
    ....
  82. ncbi Linezolid in methicillin-resistant Staphylococcus aureus nosocomial pneumonia: a randomized, controlled study
    Richard G Wunderink
    Department of Pulmonary and Critical Care, Northwestern University Feinberg School of Medicine, Chicago, Illinois 60611, USA
    Clin Infect Dis 54:621-9. 2012
    ..This study prospectively assessed efficacy and safety of linezolid, compared with a dose-optimized vancomycin regimen, for treatment of MRSA nosocomial pneumonia...
  83. ncbi Multicity outbreak of linezolid-resistant Staphylococcus epidermidis associated with clonal spread of a cfr-containing strain
    Hector Bonilla
    Summa Health System, Akron, Ohio, USA
    Clin Infect Dis 51:796-800. 2010
    ..Two clones with different mechanisms of linezolid resistance were circulating in hospital A. One of these contained the cfr gene, and the other a ribosomal mutation. The clone containing cfr was identical in both hospitals...
  84. pmc Pharmacokinetics of linezolid in subjects with renal dysfunction
    Michael E Brier
    University of Louisville, Department of Veterans Affairs, Louisville, Kentucky 40202, USA
    Antimicrob Agents Chemother 47:2775-80. 2003
    Linezolid is a member of a new, unique class of synthetic antibacterial agents called oxazolidinones that are effective against gram-positive bacteria, including vancomycin-resistant organisms...
  85. ncbi Design of the DEFINE trial: determining the EFficacy and tolerability of CETP INhibition with AnacEtrapib
    Christopher P Cannon
    TIMI Study Group, Cardiovascular Division, Brigham and Women s Hospital, Boston, MA 02115, USA
    Am Heart J 158:513-519.e3. 2009
    ..Adverse effects on blood pressure, electrolytes, and aldosterone levels, seen with another drug in this class, have not been noted in studies of anacetrapib to date...
  86. ncbi Linezolid: the first oxazolidinone antimicrobial
    Robert C Moellering
    Department of Medicine, Beth Israel Deaconess Medical Center, Boston, Massachusetts 02215, USA
    Ann Intern Med 138:135-42. 2003
    Linezolid is the first of a new class of antimicrobial agents, the oxazolidinones, to be approved for clinical use in the United States and elsewhere...
  87. ncbi Linezolid versus ceftriaxone/cefpodoxime in patients hospitalized for the treatment of Streptococcus pneumoniae pneumonia
    Gerry S San Pedro
    Department of Internal Medicine, Section of Pulmonary and Critical Care Medicine, Louisiana State University Medical Center, Shreveport 71130 3932, USA
    Scand J Infect Dis 34:720-8. 2002
    ..v./oral linezolid was more effective than ceftriaxone/cefpodoxime in patients hospitalized with CAP, with comparable cure rates in S. pneumoniae pneumonia and higher cure rates in pneumonia complicated by bacteremia...
  88. ncbi Efficacy and safety of linezolid compared with vancomycin in a randomized, double-blind study of febrile neutropenic patients with cancer
    Branimir Jaksic
    Department of Medicine, Merkur University Hospital, Zagreb, Croatia
    Clin Infect Dis 42:597-607. 2006
    ..Gram-positive pathogens can cause serious infections in neutropenic patients with cancer, and vancomycin therapy is often initiated empirically. Linezolid may offer an option for these patients...
  89. ncbi Efficacy and safety of tigecycline compared with vancomycin or linezolid for treatment of serious infections with methicillin-resistant Staphylococcus aureus or vancomycin-resistant enterococci: a Phase 3, multicentre, double-blind, randomized study
    I Florescu
    Emergency Clinical Hospital, Bucharest, Romania
    J Antimicrob Chemother 62:i17-28. 2008
    ..Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE) are causing serious nosocomial infections. Tigecycline was evaluated in hospitalized patients with MRSA or VRE infection...
  90. ncbi The herbicide ketoclomazone inhibits 1-deoxy-D-xylulose 5-phosphate synthase in the 2-C-methyl-D-erythritol 4-phosphate pathway and shows antibacterial activity against Haemophilus influenzae
    Yukiko Matsue
    Biotechnology Research Center, The University of Tokyo, 1 1 1 Yayoi, Bunkyo ku, Tokyo, Japan
    J Antibiot (Tokyo) 63:583-8. 2010
    ..These data reveal the inhibitory mechanism of ketoclomazone on DXP synthase...
  91. ncbi In vitro activity of linezolid in combination with doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin against methicillin-susceptible Staphylococcus aureus
    J M Sahuquillo Arce
    Department of Clinical Microbiology, Hospital La Fe, Avda Campanar 21, 46009 Valencia, Spain
    Rev Esp Quimioter 19:252-7. 2006
    ..In summary, the combination of subinhibitory...
  92. ncbi Nosocomial outbreak of linezolid-resistant Enterococcus faecalis infection in a tertiary care hospital
    Rosa Gómez-Gil
    Servicio de Microbiología y Parasitología and Unidad de Investigación, Hospital Universitario La Paz, 28046 Madrid, Spain
    Diagn Microbiol Infect Dis 65:175-9. 2009
    ....
  93. ncbi Linezolid versus vancomycin or teicoplanin for nosocomial pneumonia: a systematic review and meta-analysis
    Andre C Kalil
    University of Nebraska Medical Center, Omaha, NE, USA
    Crit Care Med 38:1802-8. 2010
    ..However, clinical superiority has not been demonstrated...
  94. pmc Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations
    Jeffrey B Locke
    Trius Therapeutics, Inc, 6310 Nancy Ridge Drive, Suite 101, San Diego, CA 92121, USA
    Antimicrob Agents Chemother 54:5337-43. 2010
    ..activity against LZD-resistant (LZD(r)) strains, we compared structurally diverse, clinically relevant oxazolidinones, including LZD, radezolid (RX-1741), TR-700 (torezolid), and a set of TR-700 analogs (including novel CD-rings ..
  95. ncbi Linezolid-associated peripheral and optic neuropathy, lactic acidosis, and serotonin syndrome
    Masashi Narita
    Infectious Disease Section, University of Pittsburgh, Veterans Affairs Pittsburgh Healthcare System, Pittsburgh, Pennsylvania 15240, USA
    Pharmacotherapy 27:1189-97. 2007
    ..Linezolid should be discontinued immediately in patients experiencing these adverse effects. Patients receiving linezolid for more than 28 days should be monitored for signs of peripheral and optic neuropathy...
  96. ncbi Zolmitriptan: a review of its use in migraine
    C M Spencer
    Adis International Limited, Auckland, New Zealand
    Drugs 58:347-74. 1999
    ..The most common adverse events with zolmitriptan therapy are asthenia, heaviness other than that of the chest or neck, dry mouth, nausea, dizziness, somnolence, paraesthesia, warm sensation, tightness, vasodilation and chest pain...
  97. pmc Pharmacokinetics and tissue penetration of linezolid following multiple oral doses
    T Gee
    Department of Microbiology, City Hospital NHS Trust, Birmingham, B18 7QH, United Kingdom
    Antimicrob Agents Chemother 45:1843-6. 2001
    ..3 (SD, 73.1) and 155.3 (SD, 80.1) microg x h/ml, respectively. These data suggest that linezolid has good tissue penetration, and we can predict that it will be successful in the treatment of a variety of gram-positive infections...
  98. ncbi Linezolid and vancomycin in treatment of lower-extremity complicated skin and skin structure infections caused by methicillin-resistant Staphylococcus aureus in patients with and without vascular disease
    Therese M Duane
    Department of Surgery, Virginia Commonwealth University, Richmond, Virginia, USA
    Surg Infect (Larchmt) 13:147-53. 2012
    ....
  99. pmc Biochemical characterization of cholesteryl ester transfer protein inhibitors
    Mollie Ranalletta
    Merck Research Laboratories, Rahway, NJ 07065, USA
    J Lipid Res 51:2739-52. 2010
    ..Each CETP inhibitor induced tight binding of CETP to HDL, indicating that these inhibitors promote the formation of a complex between CETP and HDL, resulting in inhibition of CETP activity...
  100. ncbi Effect of linezolid on cytokine production capacity and plasma endotoxin levels in response to lipopolysaccharide stimulation of whole blood
    Gaku Takahashi
    Department of Critical Care Medicine, Iwate Medical University, School of Medicine, 19 1 Uchimaru, Morioka, 020 8505, Japan
    J Infect Chemother 16:94-9. 2010
    ..The results indicate that LZD may have a significant role in saving the lives of patients with sepsis...
  101. ncbi Effect of linezolid versus vancomycin on length of hospital stay in patients with complicated skin and soft tissue infections caused by known or suspected methicillin-resistant staphylococci: results from a randomized clinical trial
    Jim Zhiming Li
    Pharmacia Corporation, Kalamazoo, Michigan 49001, USA
    Surg Infect (Larchmt) 4:57-70. 2003
    ..To determine if oral linezolid can reduce length of hospital stay (LOS) when compared to vancomycin, we compared the LOS for the 230 complicated skin and soft tissue infection patients enrolled in this trial...

Research Grants49

  1. Targeting a novel regulatory RNA with novel antibiotics
    Jennifer V Hines; Fiscal Year: 2010
    ..Our hypothesis is that the proposed new classes of oxazolidinones and related compounds can be developed into novel antibacterial agents and that the T box antitermination ..
  2. Effecting C-O activation of oxazolidinones by Ni to construct small, chiral heter
    MATTHEW STEVEN WINSTON; Fiscal Year: 2012
    DESCRIPTION (provided by applicant): Given their wide availability, chiral oxazolidinones are potentially useful but ignored substrates for catalysis...
  3. Hygromycin A: Activity, Biosynthesis, Export, Resistance and Regulation
    Kevin A Reynolds; Fiscal Year: 2013
    ..macrolides (azithromycin, telithromycin), tetracyclines, aminoglycosides (gentamycin), and more recently oxazolidinones (linezolid) target the bacterial ribosome, which is essential for intracellular protein synthesis...
  4. ANTIBIOTIC INHIBITION OF BACTERIAL RIBOSOME FORMATION
    WILLIAM CHAMPNEY; Fiscal Year: 2002
    ..observation that macrolide antibiotics as well as the ketolides, lincosamides, streptogramin B compounds and oxazolidinones can all inhibit the assembly of the large ribosomal subunit in bacterial cells...
  5. ASYMMETRIC SYNTHESIS OF ANTITUMOR AGENTS
    MICHAEL CRIMMINS; Fiscal Year: 2005
    ..Laulimalide stimulates tubulin polymerization more effectively than paclitaxel. Laulimalide is a representative of a new class of microtubule stabilizing agents with promise for therapeutic potential. ..
  6. Micromass LCT Mass Spectrometer
    MICHAEL CRIMMINS; Fiscal Year: 2004
    ..The major users group is highly dependent on rapid turn around mass spectral data. Since there is currently no Departmental mass spectrometry facility, the research programs of the major users have been seriously hampered for some time. ..
  7. ASYMMETRIC SYNTHESIS OF NOVEL NATURAL PRODUCTS
    MICHAEL CRIMMINS; Fiscal Year: 2006
    ..Synthesis of the biologically active agents guanacastepene, and SCH 351448 will also be pursued. ..
  8. Chemical and Biological Studies on Biaryl Phenolics
    Ken Feldman; Fiscal Year: 2005
    ..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..
  9. Alkynyliodonium Salts and Derived Diyls in Synthesis
    Ken Feldman; Fiscal Year: 2009
    ..abstract_text> ..
  10. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  11. Detection of Biofilm Bacteria using GloBac
    Robin Patel; Fiscal Year: 2008
    ..The goal of the proposed studies is to develop a rapid test for detection of bacteria on artificial joints that can be used in the operating room to diagnose infected artificial joints. [unreadable] [unreadable] [unreadable]..
  12. Enhancement of antimicrobics by electrical current
    Robin Patel; Fiscal Year: 2007
    ..This novel but simple resistance reversing strategy may generalize to a wide variety of antimicrobics and microorganisms and a wide variety of biofilm-associated human infections. [unreadable] [unreadable] [unreadable] [unreadable]..
  13. New Methodology for Indole Alkaloid Syntheses
    Ken S Feldman; Fiscal Year: 2010
    ..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. ..
  14. HUMAN RETROVIRUS-5 AND ARTHRITIS
    Robin Patel; Fiscal Year: 2002
    ..Identification of a specific infectious agent associated with these arthritides would potentially allo for the development of preventive strategies such as vaccination and novel therapeutic approaches. ..
  15. SK Channel Openers as Therapeutics for Cerebellar Ataxia
    Heike Wulff; Fiscal Year: 2007
    ..Taken together these important proof-of-concept studies will help to determine whether SK channel openers constitute a new therapeutic approach to improve motor performance in dominant cerebellar ataxias. ..
  16. Migraine Pathophysiology:Thalamus and Extended Allodynia
    Rami Burstein; Fiscal Year: 2009
    ....
  17. Asymmetric Synthesis of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2007
    ..The photodesulfmylation of sulfinamides represents an important new protocol, not requiring acids or bases, for the removal of the valuable amine N-sulfinyl protecting group. ..
  18. Evolutionary Dissection of complex traits
    Stephen Wooding; Fiscal Year: 2008
    ..By applying a combined evolutionary and epidemiological approach, these analyses may shed new light on the relationship between genetic variation, environmental response, and human health. [unreadable] [unreadable] [unreadable]..
  19. Synthesis of Polyketides and Terpenes
    David A Evans; Fiscal Year: 2010
    ..As a consequence, organic synthesis is a critical discipline that continues to have an important impact on the fields of both medicine and biology. ..
  20. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2009
    ..Daphnicyclidin A. This recent discovery has revealed a new molecular architecture which exhibits significant antitumor activity. Our research will investigate strategies for chemical synthesis of these complex polycyclic systems. ..
  21. New mechanism of resistance to oxazolidinone antibiotics in Staphylococcus aureus
    Alexander S Mankin; Fiscal Year: 2010
    ....
  22. Molecular Target Focused Discovery of Anticancer Drugs
    George R Pettit; Fiscal Year: 2010
    ....
  23. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  24. Reducing Antimicrobial Use Associated with Ventilator Associated Pneumonia and Ca
    SARA ELIZABETH COSGROVE; Fiscal Year: 2010
    ..We hypothesize that this approach will enhance appropriate use of antimicrobials for both VAP and CAUTI and improve patient outcomes by reducing the known sequelae of antimicrobial overuse. ..
  25. Legionella pneumophila developmental cycle & virulence
    PAUL STOKES HOFFMAN; Fiscal Year: 2011
    ..These studies should also provide insights relevant to other opportunistic environmental pathogens including oxiella, Burkholderia and species of Mycobacterium. ..
  26. Catheter Dwell Time and Risk of Bloodstream Infections in Hospitalized Neonates
    Aaron M Milstone; Fiscal Year: 2011
    ..This project will help to develop evidence-based strategies to prevent bloodstream infections among vulnerable infants hospitalized in the neonatal intensive care unit. ..
  27. Defining Moxifloxacin as a First-line TB Drug
    Eric Nuermberger; Fiscal Year: 2008
    ..Relevance: Results of these studies will help to define optimal treatment regimens for TB that can be used to design new clinical trials or, in some cases, directly applied to clinical practice. ..
  28. PSYCHOMOTOR STIMULANTS AND AGGRESSION IN ANIMALS
    KLAUS MICZEK; Fiscal Year: 2008
    ..Reversal of cross-sensitization from stress may be a means by which to prevent the transition to out-of-control compulsive-like drug taking. ..
  29. Study of a New Class of Chiral Nucleophilic Catalysts
    VLADIMIR BIRMAN; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  30. Antibiotic Hypersusceptibility Mutations in Bacteria
    Alexander Mankin; Fiscal Year: 2005
    ..In addition to identifying promising targets for potentiators, the project will help unravel new aspects of the mechanism of action of antibiotics and new features of bacterial physiology. ..
  31. NEUROBIOLOGY OF ANOREXIA INDUCED BY MIGRAINE PAIN
    Rami Burstein; Fiscal Year: 2004
    ..abstract_text> ..
  32. ALCOHOL BENZODIAZEPHINES AND AGGRESSION IN ANIMALS
    KLAUS MICZEK; Fiscal Year: 2002
    ....
  33. COMPARATIVE GENOMIC ANALYSIS OF CARDIOVASCULAR GENE REGU
    Ronald Krauss; Fiscal Year: 2003
    ..6) The establishment of an educational program for cardiovascular researchers in the use of genomic databases and tools. ..
  34. RIBOSOMAL PEPTIDYL TRANSFERASE CENTER
    Alexander Mankin; Fiscal Year: 2003
    ..Understanding structure and function of the main catalytic center of the ribosome is indispensable for the rational design of new antibiotics and overcoming mechanisms of drug resistance. ..
  35. SYNTHESIS OF BIOACTIVE MACROLIDES
    James White; Fiscal Year: 2002
    ..These pathways, regardless of whether they are successful, must also serve as paradigms for accessing other potentially useful chemotherapeutic agents of equal or greater complexity. ..
  36. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 2001
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  37. Chemokines and microglia in Alzheimer's disease
    Joseph El Khoury; Fiscal Year: 2005
    ....
  38. Syntheses of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2005
    ..Targets include cyclic, unsaturated, and, beta substituted derivatives (beta amino, beta hydroxy, and beta fluoro). ..
  39. Transmission Dynamics of Antimocrobial-resistant bacteria in dialysis units
    ERIKA D AGATA; Fiscal Year: 2007
    ..Limiting ARB spread will ultimately reduce infections caused by ARB and improve CHD patient outcomes. [unreadable] [unreadable] [unreadable]..
  40. Molecular Target Focused Discovery of Anticancer Drugs
    GEORGE PETTIT; Fiscal Year: 2007
    ..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
  41. Small Molecule Kv1.3 Blockers as New Therapeutics for Multiple Sclerosis
    Heike Wulff; Fiscal Year: 2007
    ..Lay: In multiple sclerosis the immune system attacks proteins in the brain of afflicted patients. The aim of this study is to identify and test new drugs that can suppress the white blood cells that are invading the brain. ..
  42. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  43. SYNTHESIS OF BIOACTIVE ALKALOIDS
    James White; Fiscal Year: 2006
    ..A plan is presented for the synthesis of this complex heptacyclic molecule which envisions a thio-Claisen rearrangement as the key step for building the vicinal quaternary carbons of this structure. ..
  44. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
    ....
  45. Asymmetric Synthesis of Bioactive Chiral Amines
    GREGORY FRIESTAD; Fiscal Year: 2006
    ..In the long term, these endeavors will advance the art and science of synthetic organic chemistry toward the ideal of efficiency, a long-term goal which remains mostly inaccessible in syntheses of complex natural products. ..
  46. ASYMMETRIC SYNTHESIS OF IONOPHORE/MACROLIDE ANTIBIOTICS
    David Evans; Fiscal Year: 2005
    ..Our goal has been to set in place all of the reactions necessary for the rapid assemblage of any polyketide target structure. ..
  47. ACYCLIC STEREOCONTROL IN RADICAL REACTIONS
    MUKUND SIBI; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  48. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..