keyword
MENU ▼
Read by QxMD icon Read
search

oxazolidinone

keyword
https://www.readbyqxmd.com/read/28209400/multidrug-resistant-enterococcal-infections-new-compounds-novel-antimicrobial-therapies
#1
REVIEW
Roel M van Harten, Rob J L Willems, Nathaniel I Martin, Antoni P A Hendrickx
Over the past two decades infections due to antibiotic-resistant bacteria have escalated world-wide, affecting patient morbidity, mortality, and health care costs. Among these bacteria, Enterococcus faecium and Enterococcus faecalis represent opportunistic nosocomial pathogens that cause difficult-to-treat infections because of intrinsic and acquired resistance to a plethora of antibiotics. In recent years, a number of novel antimicrobial compound classes have been discovered and developed that target Gram-positive bacteria, including E...
February 13, 2017: Trends in Microbiology
https://www.readbyqxmd.com/read/28197728/linezolid-resistant-enterococci-in-polish-hospitals-species-clonality-and-determinants-of-linezolid-resistance
#2
I Gawryszewska, D Żabicka, W Hryniewicz, E Sadowy
The significant increase of the linezolid-resistant enterococci (LRE) has been observed in Polish hospitals since 2012 and our study aimed at elucidating the possible reasons for this phenomenon. Polish LRE isolates were analysed by multilocus-sequence typing (MLST) and multiple locus variable-number tandem repeat (VNTR) analysis (MLVA), polymerase chain reaction (PCR) and PCR-restriction fragment length polymorphism (PCR-RFLP) to establish clonal relatedness and mechanism of linezolid resistance, respectively...
February 14, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28197303/optimization-of-3-pyrimidin-4-yl-oxazolidin-2-ones-as-allosteric-and-mutant-specific-inhibitors-of-idh1
#3
Julian R Levell, Thomas Caferro, Gregg Chenail, Ina Dix, Julia Dooley, Brant Firestone, Pascal D Fortin, John Giraldes, Ty Gould, Joseph D Growney, Michael D Jones, Raviraj Kulathila, Fallon Lin, Gang Liu, Arne Mueller, Simon van der Plas, Kelly Slocum, Troy Smith, Remi Terranova, B Barry Touré, Viraj Tyagi, Trixie Wagner, Xiaoling Xie, Ming Xu, Fan S Yang, Liping X Zhou, Raymond Pagliarini, Young Shin Cho
High throughput screening and subsequent hit validation identified 4-isopropyl-3-(2-((1-phenylethyl)amino)pyrimidin-4-yl)oxazolidin-2-one as a potent inhibitor of IDH1(R132H). Synthesis of the four separate stereoisomers identified the (S,S)-diastereomer (IDH125, 1f) as the most potent isomer. This also showed reasonable cellular activity and excellent selectivity vs IDH1(wt). Initial structure-activity relationship exploration identified the key tolerances and potential for optimization. X-ray crystallography identified a functionally relevant allosteric binding site amenable to inhibitors, which can penetrate the blood-brain barrier, and aided rational optimization...
February 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28193240/substitution-of-ethambutol-with-linezolid-during-the-intensive-phase-of-treatment-of-pulmonary-tuberculosis-study-protocol-for-a-prospective-multicenter-randomized-open-label-phase-ii-trial
#4
Ji Yeon Lee, Deog Kyeom Kim, Jung-Kyu Lee, Ho Il Yoon, Ina Jeong, Eunyoung Heo, Young Sik Park, Jae Ho Lee, Sung Soo Park, Sang-Min Lee, Chang-Hoon Lee, Jinwoo Lee, Sun Mi Choi, Jong Sun Park, Joon-Sung Joh, Young-Jae Cho, Yeon Joo Lee, Se Joong Kim, Young Ran Hwang, Hyeonjeong Kim, Jongeun Ki, Hyungsook Choi, Jiyeon Han, Heejung Ahn, Seokyung Hahn, Jae-Joon Yim
BACKGROUND: Linezolid, an oxazolidinone, substantially improves treatment outcomes of multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis. We started a trial to test whether the use of linezolid instead of ethambutol could increase the rate of sputum culture conversion as of 8 weeks of treatment in patients with drug-susceptible tuberculosis. METHODS/DESIGN: This is a phase II, multicenter, randomized study with three arms. We are enrolling patients with pulmonary tuberculosis without rifampicin resistance screened by the Xpert MTB/RIF® assay...
February 13, 2017: Trials
https://www.readbyqxmd.com/read/28187378/development-of-an-analytical-method-for-detecting-nitrofurans-in-bee-pollen-by-liquid-chromatography-electrospray-ionization-tandem-mass-spectrometry
#5
Mi Sun Park, Kyung Tae Kim, Jong Seong Kang
Bee pollen collected by honeybees, which is in powdered form, is a good nutritional supplement. Nitrofuran antibiotics are assumed not to be present in bee pollen, which is important as the level of antibiotics in bee pollen is strongly regulated in many countries. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to detect nitrofurans in honey has been developed, but this method is not suitable for bee pollen because of it being in powdered form. During preparation of bee pollen samples, the dispersal of powder particles in an aqueous solution often makes them susceptible to forming an emulsion with solvent components such as hexane and ethyl acetate...
January 9, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28168646/synthesis-of-lactones-and-other-heterocycles
#6
REVIEW
Xi Liu, Liang-Nian He
Chemical fixation of CO2 into value-added chemicals represents a promising field in view of sustainable development and green synthesis. In this aspect, the construction of heterocyclic compounds from CO2 and readily available starting materials is particularly appealing in both organic and pharmaceutical fields since CO2 can be regarded as carbon and oxygen resource with advantages of abundance, renewability, non-toxicity, and non-flammability. In this chapter, we have summarized elegant protocols with elaborately designed substrates for the direct incorporation of entire CO2 molecule or "CO" or "C" fragments into lactones and other heterocycles such as oxazolidinones, cyclic carbonates, quinazoline-2,4(1H,3H)-diones, etc...
April 2017: Topics in Current Chemistry (Journal)
https://www.readbyqxmd.com/read/28167545/single-and-multiple-dose-study-to-determine-the-safety-tolerability-pharmacokinetics-and-food-effect-of-oral-mrx-i-versus-linezolid-in-healthy-adult-subjects
#7
Paul B Eckburg, Yigong Ge, Barry Hafkin
A multipart Phase 1 study was conducted to determine the safety, tolerability, pharmacokinetics, and food effect of the novel oral oxazolidinone, MRX-I, in healthy adults, as well as the tolerability of longer-term exposure of both oral MRX-I and linezolid.Thirty subjects in Part 1 received single ascending doses of MRX-I or placebo under fasting or fed condition in a double-blind crossover design. Twelve subjects in Part 2, received MRX-I 800 mg q12h for 14 days in double-blind, placebo-controlled design. In Part 3, 24 subjects were randomized to receive 28 days of MRX-I 800 mg q12h or oral linezolid 600 mg q12h for 28 days in a double-blind, double-dummy design...
February 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28154311/synthesis-of-linezolid-metabolites-pnu-142300-and-pnu-142586-toward-the-exploration-of-metabolite-related-events
#8
Kengo Hanaya, Kazuaki Matsumoto, Yuta Yokoyama, Junko Kizu, Mitsuru Shoji, Takeshi Sugai
Linezolid (1) is an oxazolidinone antibiotic that is partially metabolized in vivo via ring cleavage of its morpholine moiety to mainly form two metabolites, PNU-142300 (2) and PNU-142586 (3). It is supposed that accumulation of 2 and 3 in patients with renal insufficiency may cause thrombocytopenia, one of the adverse effects of linezolid. However, the poor availability of 2 and 3 has hindered further investigation of the clinical significance of the accumulation of these metabolites. In this paper, we synthesized metabolites 2 and 3 via a common synthetic intermediate, 4; this will encourage further exploration of events related to these metabolites and lead to improved clinical use of linezolid...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28140693/pharmacokinetic-drug-evaluation-of-tedizolid-for-the-treatment-of-skin-infections
#9
Darrell McBride, Tamara Krekel, Kevin Hsueh, Michael J Durkin
Tedizolid is indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI). Although tedizolid shares many similar properties with linezolid, another oxazolidinone used to treat ABSSSI, the two antibiotics have several key differences. Areas covered: This review provides a detailed summary of the overall pharmacodynamics, pharmacokinetics, clinical efficacy, and safety of tedizolid for the treatment of ABSSSI. Expert opinion: Compared to other antibiotics used for ABSSSI, tedizolid has several advantages...
March 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28137816/effects-of-tedizolid-phosphate-on-survival-outcomes-and-suppression-of-production-of-staphylococcal-toxins-in-a-rabbit-model-of-mrsa-necrotizing-pneumonia
#10
Vien T M Le, Hoan N Le, Marcos Gabriel Pinheiro, Kenneth J Hahn, Mary L Dinh, Kajal B Larson, Shawn D Flanagan, Cedric Badiou, Gerard Lina, Christine Tkaczyk, Bret R Sellman, Binh An Diep
The protective efficacy of tedizolid phosphate, a second-generation oxazolidinone that potently inhibits bacterial protein synthesis, was compared to those of linezolid, vancomycin, or saline in a rabbit model of Staphylococcus aureus necrotizing pneumonia. A rabbit dosing regimen of 6 mg/kg tedizolid phosphate IV twice daily, which yielded AUC0-24h values approximating those in humans, was used. Overall survival rate was 83% for rabbits treated with 6 mg/kg tedizolid phosphate twice daily and 83% for those treated with 50 mg/kg linezolid thrice daily (P=0...
January 30, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28134678/what-is-new-in-the-management-of-skin-and-soft-tissue-infections-in-2016
#11
Garyphallia Poulakou, Efthymia Giannitsioti, Sotirios Tsiodras
PURPOSE OF REVIEW: Skin and soft tissue infections (SSTIs) are the most frequent infectious cause of referrals to emergency departments and hospital admissions in developed world, contributing to significant morbidity and healthcare expenditures. We sought to review recent literature covering epidemiology and management of SSTIs. RECENT FINDINGS: Incidence trends of SSTIs were increasing worldwide with Staphylococcus aureus and streptococci predominating and methicillin-resistant S...
January 27, 2017: Current Opinion in Infectious Diseases
https://www.readbyqxmd.com/read/28129816/-update-on-antibiotic-resistance-in-gram-positive-bacteria
#12
Carmen Lozano, Carmen Torres
Antimicrobial resistance among Gram-positive bacteria, especially in Staphylococcus aureus, Enterococcus faecium, Enterococcus faecalis, and Streptococcus pneumoniae, is a serious threat to public health. These microorganisms have multiple resistance mechanisms to agents currently used in clinical practice. Many of these resistance mechanisms are common to all 4 of these bacterial species, but other mechanisms seem to be more specific. The prevalence and dissemination of these mechanisms varies considerably, depending on the microorganism...
January 2017: Enfermedades Infecciosas y Microbiología Clínica
https://www.readbyqxmd.com/read/28127613/recent-advances-in-reactions-of-aryl-sulfonyl-isocyanates
#13
REVIEW
Dayun Huang, Guobing Yan
Aryl sulfonyl isocyanates are important intermediates in organic synthesis. They are used as electrophilic reagents and easily react with nucleophiles to form amides, sulfonyl ureas, pyrrolidine derivatives, lactams, oxazolidinones, and so on. Although there are some reviews on the applications of isocyanates in chemistry, few are concerned about aryl sulfonyl isocyanates. This review focuses on recent advances related to aryl sulfonyl isocyanates in organic synthesis, mainly including three special characteristics...
January 27, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28118218/obesity-and-skin-and-soft-tissue-infections-how-to-optimize-antimicrobial-usage-for-prevention-and-treatment
#14
Mordechai Grupper, David P Nicolau
PURPOSE OF REVIEW: Skin and soft tissue infections (SSTIs) are prevalent in the obese population, with rising trend expected. Although numerous antibiotics are available for the prevention and treatment of SSTIs, their characterization in obese patients is not a regulatory mandate. Consequently, information that carries importance for optimizing the dosing regimen in the obese population may not be readily available. This review focuses on the most recent pharmacokinetic and pharmacodynamic data on this topic with attention to cefazolin for surgical prophylaxis as well as antibiotics that are active against methicillin-resistant Staphylococcus aureus (MRSA)...
January 23, 2017: Current Opinion in Infectious Diseases
https://www.readbyqxmd.com/read/28106208/studies-on-cyclization-reactions-of-3-amino-2-4-dihydroxybutanoic-acid-derivatives
#15
Mathieu Esgulian, Vincent Belot, Régis Guillot, Sandrine Deloisy, David J Aitken
A number of cyclic derivatives of 3-amino-2,4-dihydroxybutanoic acid are known in the literature but they are often prepared from other cyclic precursors. This study showed that the title compound too may serve as a convenient substrate for cyclization reactions. Using orthogonally-protected linear derivatives, regioselective cyclizations were performed, leading to original and highly-functionalized γ-lactones, oxazolidinones, oxazolines and aziridines. In these reactions a key role was played by the C3 nitrogen group function, while the C2 alcohol function showed no propensity for participation in cyclization reactions...
January 20, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28080036/lithium-hexamethyldisilazide-mediated-enolization-of-acylated-oxazolidinones-solvent-cosolvent-and-isotope-effects-on-competing-monomer-and-dimer-based-pathways
#16
Gabriel J Reyes-Rodríguez, Russell F Algera, David B Collum
Lithium hexamethyldisilazide (LiHMDS)-mediated enolization of (+)-4-benzyl-3-propionyl-2-oxazolidinone in THF-hydrocarbon mixtures shows unusual sensitivity to the choice of hydrocarbon cosolvent (hexane versus toluene) and to isotopic labeling. Four mechanisms corresponding to monosolvated monomers, trisolvated dimers, octasolvated monomers, and octasolvated dimers were identified. Even under conditions in which the LiHMDS monomer was the dominant observable form, dimer-based metalation was significant. The mechanism-dependent isotope and cosolvent effects are discussed in the context of ground-state stabilization and transition-state tunneling...
January 12, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28077022/feasibility-of-a-novel-multispot-nanoarray-for-antibiotic-screening-in-honey
#17
Sara E McNamee, Giulia Rosar, Lidija Persic, Christopher T Elliott, Katrina Campbell
Practical solutions for multiple antibiotic determination in food is required by the food industry and regulators for cost effective screening purposes. This study describes the feasibility in development and preliminary performance of a novel multispot nanoarray for antibiotic screening in honey. Using a multiplex approach the metabolites of the four main nitrofuran antibiotics including morpholinomethyl-2-oxazolidone (AMOZ), 3-amino-2-oxazolidinone (AOZ), semicarbazide (SEM), 1-aminohydantoin (AHD) and chloramphenicol (CAP) were simultaneously detected...
January 12, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28049370/underlying-molecular-interaction-of-bovine-serum-albumin-and-linezolid-a-biophysical-outlook
#18
Amartya Roy, Paromita Seal, Jyotirmoy Sikdar, Sanghamitra Banerjee, Rajen Haldar
Linezolid, one of the reserve antibiotic of oxazolidinone class has wide range of antimicrobial activity. Here we have conducted a fundamental study concerning the dynamics of its interaction with bovine serum albumin (BSA), and the post binding modification of the later by employing different spectroscopic (absorption, fluorescence and circular dichroism (CD) spectroscopy) and molecular docking tools. Gradual quenching of the tryptophan (Trp) fluorescence upon addition of linezolid to BSA confirms their interaction...
January 19, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27999068/linezolid-a-promising-option-in-the-treatment-of-gram-positives
#19
Abed Zahedi Bialvaei, Mohammad Rahbar, Mehdi Yousefi, Mohammad Asgharzadeh, Hossein Samadi Kafil
Linezolid, an oxazolidinone antimicrobial agent that acts by inhibiting protein synthesis in a unique fashion, is used in the treatment of community-acquired pneumonia, skin and soft-tissue infections and other infections caused by Gram-positive bacteria including VRE and methicillin-resistant staphylococci. Currently, linezolid resistance among these pathogens remains low, commonly <1.0%, although the prevalence of antibiotic resistance is increasing in many countries. Therefore, the development of resistance by clinical isolates should prompt increased attention of clinical laboratories to routinely perform linezolid susceptibility testing for this important agent and should be taken into account when considering its therapeutic use...
February 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/27999045/emergence-and-dissemination-of-a-linezolid-resistant-staphylococcus-capitis-clone-in-europe
#20
M Butin, P Martins-Simões, B Pichon, D Leyssene, S Bordes-Couecou, H Meugnier, C Rouard, N Lemaitre, F Schramm, A Kearns, I Spiliopoulou, H-L Hyyryläinen, O Dumitrescu, F Vandenesch, C Dupieux, F Laurent
OBJECTIVES: We investigated the epidemiological, clinical, microbiological and genetic characteristics of linezolid-resistant (LZR) Staphylococcus capitis isolates from French ICUs, and compared them with LZR S. capitis isolates from other European countries. METHODS: All LZR isolates were subjected to antimicrobial susceptibility testing (AST) and the presence of cfr and optrA genes as well as mutations in the 23S rRNA and ribosomal proteins were investigated using specific PCR with sequencing...
December 20, 2016: Journal of Antimicrobial Chemotherapy
keyword
keyword
103902
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"