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oxazolidinone

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https://www.readbyqxmd.com/read/28432878/in-vitro-susceptibility-of-methicillin-resistant-staphylococcus-aureus-isolates-from-skin-and-soft-tissue-infections-to-vancomycin-daptomycin-linezolid-and-tedizolid
#1
Johanna Marcela Vanegas Múnera, Ana María Ocampo Ríos, Daniela Montoya Urrego, Judy Natalia Jiménez Quiceno
INTRODUCTION: Treatment of multidrug-resistant Gram-positive infections caused by Staphylococcus aureus remains as a clinical challenge due to emergence of new resistance mechanisms. Tedizolid is a next-generation oxazolidinone, recently approved for skin and soft tissues infections. We conducted a study to determine in vitro susceptibility to vancomycin, daptomycin, linezolid, and tedizolid in MRSA clinical isolates from adult patients with skin and soft tissue infections. MATERIAL AND METHODS: Methicillin-resistant S...
April 19, 2017: Brazilian Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28428726/successful-treatment-of-prosthetic-joint-infection-due-to-vancomycin-resistant-enterococci-with-tedizolid
#2
Sheng Si, Michael J Durkin, Maureen M Mercier, Melanie L Yarbrough, Stephen Y Liang
Few antibiotic options exist for the management of infections due to vancomycin-resistant enterococci (VRE). We describe a case involving the safe and successful use of tedizolid, a new oxazolidinone, to treat VRE prosthetic joint infection.
March 2017: Infectious Diseases in Clinical Practice: IDCP
https://www.readbyqxmd.com/read/28427814/design-synthesis-and-x-ray-structural-studies-of-bace-1-inhibitors-containing-substituted-2-oxopiperazines-as-p1-p2-ligands
#3
Arun K Ghosh, Margherita Brindisi, Yu-Chen Yen, Emilio L Cárdenas, Jean-Rene Ella-Menye, Nagaswamy Kumaragurubaran, Xiangping Huang, Jordan Tang, Andrew D Mesecar
We report the design and synthesis of a series of BACE1 inhibitors incorporating mono- and bicyclic 6-substituted 2-oxopiperazines as novel P1' and P2' ligands and isophthalamide derivative as P2-P3 ligands. Among mono-substituted 2-oxopiperazines, inhibitor 5a with N-benzyl-2-oxopiperazine and isophthalamide showed potent BACE1 inhibitory activity (Ki=2nM). Inhibitor 5g, with N-benzyl-2-oxopiperazine and substituted indole-derived P2-ligand showed a reduction in potency. The X-ray crystal structure of 5g-bound BACE1 was determined and used to design a set of disubstituted 2-oxopiperazines and bicyclic derivatives that were subsequently investigated...
April 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28422263/synthesis-of-oxazolidinones-rhodium-catalyzed-c-h-amination-of-n-mesyloxycarbamates
#4
Hélène Lebel, Laura Mamani Laparra, Maroua Khalifa, Carl Trudel, Clément Audubert, Mathieu Szponarski, Cédric Dicaire Leduc, Emna Azek, Matthias Ernzerhof
N-Mesyloxycarbamates undergo intramolecular C-H amination reactions to afford oxazolidinones in good to excellent yields in the presence of rhodium(ii) carboxylate catalysts. The reaction is performed under green conditions and potassium carbonate is used, forming biodegradable potassium mesylate as a reaction by-product. This method enables the production of electron-rich, electron-deficient, aromatic and heteroaromatic oxazolidinones in good to excellent yields. Conformationally restricted cyclic secondary N-mesyloxycarbamates furnish cis-oxazolidinones in high yields and selectivity; DFT calculations are provided to account for the observed selectivity...
April 19, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28362383/methodology-for-the-study-of-horizontal-gene-transfer-in-staphylococcus-aureus
#5
Fabio Cafini, Nguyen Thi Le Thuy, Federico Román, José Prieto, Sarah Dubrac, Tarek Msadek, Kazuya Morikawa
One important feature of the major opportunistic human pathogen Staphylococcus aureus is its extraordinary ability to rapidly acquire resistance to antibiotics. Genomic studies reveal that S. aureus carries many virulence and resistance genes located in mobile genetic elements, suggesting that horizontal gene transfer (HGT) plays a critical role in S. aureus evolution. However, a full and detailed description of the methodology used to study HGT in S. aureus is still lacking, especially regarding natural transformation, which has been recently reported in this bacterium...
March 10, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28330892/in-vitro-susceptibility-testing-of-tedizolid-against-nontuberculous-mycobacteria
#6
Barbara A Brown-Elliott, Richard J Wallace
Tedizolid is a new oxazolidinone with improved in vitro and intracellular potency against Mycobacterium tuberculosis, including multidrug resistant strains, and some species of nontuberculous mycobacteria (NTM) compared with linezolid.Using the current Clinical and Laboratory Standards Institute (CLSI) recommended method of broth microdilution, susceptibility testing of 170 isolates of rapidly growing mycobacteria showed equivalent or lower (1- to 8-fold MIC50 and/or MIC90 values) for tedizolid compared to linezolid...
March 22, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28314920/-new-antibiotics-standstill-or-progress
#7
J Rademacher, T Welte
The development of resistance to antibiotics has been ignored for a long time. But nowadays, increasing resistance is an important topic. For a decade no new antibiotics had been developed and it is not possible to quickly close this gap of new resistance and no new drugs. This work presents six new antibiotics (ceftaroline, ceftobiprole, solithromycin, tedizolid, ceftolozane/tazobactam, ceftazidime/avibactam). In part, only expert opinions are given due to lack of study results.The two 5th generation cephalosporins ceftaroline and ceftobiprole have beside their equivalent efficacy to ceftriaxone (ceftaroline) and cefipim (ceftobiprole) high activity against MRSA...
March 17, 2017: Medizinische Klinik, Intensivmedizin und Notfallmedizin
https://www.readbyqxmd.com/read/28284617/detection-of-novel-oxazolidinone-and-phenicol-resistance-gene-optra-in-enterococcal-isolates-from-food-animals-and-animal-carcasses
#8
Migma Dorji Tamang, Dong Chan Moon, Su-Ran Kim, Hee Young Kang, Kichan Lee, Hyang-Mi Nam, Geum-Chan Jang, Hee-Soo Lee, Suk-Chan Jung, Suk-Kyung Lim
Altogether 7720 Enterococcus faecalis and 3939 E. faecium isolated from food animals and animal carcasses during 2003-2014 in Korea were investigated to determine if linezolid-resistant (LR) enterococci (≥8μg/ml) are present. Overall, 12 E. faecalis and 27 E. faecium recovered from chickens (n=32), pigs (n=6), and cattle (n=1) were resistant to linezolid and were further characterized using molecular methods Most LR isolates were also resistant to chloramphenicol (97.44%) and florfenicol (92.31%). Molecular analysis showed no mutations in the 23S ribosomal RNA and in the ribosomal protein L3...
March 2017: Veterinary Microbiology
https://www.readbyqxmd.com/read/28279932/enantioselective-recognition-of-radezolid-by-cyclodextrin-modified-capillary-electrokinetic-chromatography-and-electronic-circular-dichroism
#9
Katarzyna Michalska, Ewa Gruba, Wojciech Bocian, Judyta Cielecka-Piontek
A method for the enantioseparation of radezolid (RAD), an analogue of a truly new class of antibacterial agents, oxazolidinones, was developed based on capillary electrokinetic chromatography using a cyclodextrin as a chiral pseudophase (CD-cEKC). The mechanism of RAD separation, together with its precursor, were investigated to directly define the relationship between the oxazolidinone structure and the complexation process. During the development of the method, anionic single isomer cyclodextrins were tested...
May 30, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28273820/in-vitro-activities-of-lcb-01-0648-a-novel-oxazolidinone-against-gram-positive-bacteria
#10
Sang-Hun Oh, Josep Kim, Sung-Yoon Baek, Sang-Eun Chae, Hee-Soo Park, Young-Lag Cho, Jin-Hwan Kwak
Oxazolidinones are a novel class of synthetic antibacterial agents that inhibit bacterial protein synthesis. Here, we synthesized and tested a series of oxazolidinone compounds containing cyclic amidrazone. Among these compounds, we further investigated the antibacterial activities of LCB01-0648 against drug-susceptible or resistant Gram-positive cocci in comparison with those of six reference compounds. LCB01-0648 showed the most potent antimicrobial activities against clinically isolated Gram-positive bacteria...
March 3, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28266144/an-experimental-and-theoretical-study-on-the-unexpected-catalytic-activity-of-triethanolamine-for-the-carboxylative-cyclization-of-propargylic-amines-with-co2
#11
Yuling Zhao, Jikuan Qiu, Zhiyong Li, Huiyong Wang, Maohong Fan, Jian Ji Wang
The chemical conversion of CO2 under atmospheric pressure and metal-free conditions remains a great challenge. In this work, a series of alkylolamines, low-cost and biodegradable bases, were used to catalyze the carboxylative cyclization of propargyl amines with CO2. It was found that among these alkylolamines, triethanolamine (TEOA) was shown to be a highly efficient organocatalyst for this important transformation at atmospheric pressure, and a series of desired products were synthesized in good to excellent yields...
March 7, 2017: ChemSusChem
https://www.readbyqxmd.com/read/28262667/integrated-co2-capture-fixation-chemistry-via-interfacial-ionic-liquid-catalyst-in-laminar-gas-liquid-flow
#12
Niraj K Vishwakarma, Ajay K Singh, Yoon-Ho Hwang, Dong-Hyeon Ko, Jin-Oh Kim, A Giridhar Babu, Dong-Pyo Kim
Simultaneous capture of carbon dioxide (CO2) and its utilization with subsequent work-up would significantly enhance the competitiveness of CO2-based sustainable chemistry over petroleum-based chemistry. Here we report an interfacial catalytic reaction platform for an integrated autonomous process of simultaneously capturing/fixing CO2 in gas-liquid laminar flow with subsequently providing a work-up step. The continuous-flow microreactor has built-in silicon nanowires (SiNWs) with immobilized ionic liquid catalysts on tips of cone-shaped nanowire bundles...
March 6, 2017: Nature Communications
https://www.readbyqxmd.com/read/28209400/multidrug-resistant-enterococcal-infections-new-compounds-novel-antimicrobial-therapies
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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 at 800 mg every 12 h (q12h) for 14 days in a double-blind, placebo-controlled design...
April 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
#20
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
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