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oxazolidinone

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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
#1
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
#2
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
#3
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 3, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27999068/linezolid-a-promising-option-in-the-treatment-of-gram-positives
#4
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...
December 20, 2016: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/27999045/emergence-and-dissemination-of-a-linezolid-resistant-staphylococcus-capitis-clone-in-europe
#5
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
https://www.readbyqxmd.com/read/27993853/in-vitro-activities-of-mcb3681-and-8-comparators-against-clostridium-difficile-isolates-with-known-ribotypes-and-diverse-geographical-spread
#6
J Freeman, S Pilling, J Vernon, M H Wilcox
Treatments for Clostridium difficile infection remain limited, despite the introduction of fidaxomicin, and development of new agents is necessary.We determined the in vitro susceptibilities of 199 prevalent or emerging Clostridium difficile PCR ribotypes to MCB3681, a novel investigational quinolonyl-oxazolidinone, and 8 comparators (metronidazole, vancomycin, fidaxomicin, moxifloxacin, ciprofloxacin, clindamycin, tigecycline and linezolid).MCB3681 showed good activity against C. difficile with no evidence of MCB3681 resistance in isolates showing either or both moxifloxacin and linezolid resistance...
December 19, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27980985/a-porous-metal-organic-framework-assembled-by-cu30-nanocages-serving-as-recyclable-catalysts-for-co2-fixation-with-aziridines
#7
Hang Xu, Xiao-Fang Liu, Chun-Shuai Cao, Bin Zhao, Peng Cheng, Liang-Nian He
Based on a novel ligand 5-(2,6-bis(4-carboxyphenyl)pyridin-4-yl)isophthalic acid (H4BCP) with large skeletons, a unique porous framework {[Cu2(BCP)(H2O)2]·3DMF} n (1) assembled by nano-sized and censer-like [Cu30] cages is successfully obtained and structurally characterized. In 1, the large 1D channel in frameworks and window size in the nanocages can enrich methylene blue and capture CO2, exhibiting the promising applications in environmental protection. More importantly, the explorations on the cycloaddition reaction of CO2 and aziridines with various substituents suggest that 1 can serve as an efficient heterogeneous catalyst for CO2 conversion with aziridines in a solvent-free system, which can be reused at least ten times without any obvious loss in catalytic activity...
November 2016: Advanced Science (Weinheim, Baden-Wurttemberg, Germany)
https://www.readbyqxmd.com/read/27979167/simultaneous-detection-of-four-nitrofuran-metabolites-in-honey-by-using-a-visualized-microarray-screen-assay
#8
Zhonghui Li, Zhoumin Li, Danke Xu
A visualized microarray sensing technique has been developed and applied to the screening of honey samples for residues of banned nitrofuran antibiotics. Using a multiplexed approach, metabolites of four main nitrofuran antibiotics can be detected simultaneously. Individual antigens were spotted onto 96-well plates. An indirective competitive assay format, with visualized signal response, was employed. An extraction method, based on derivatization with 2-nitrobenzaldehyde and partition into ethyl acetate, was used for screening...
April 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/27978473/a-validated-uplc-ms-ms-method-for-the-analysis-of-linezolid-and-a-novel-oxazolidinone-derivative-ph027-in-plasma-and-its-application-to-tissue-distribution-study-in-rabbits
#9
Mohsen A Hedaya, Vidhya Thomas, Mohamed E Abdel-Hamid, Elijah O Kehinde, Oludotun A Phillips
OBJECTIVES: Linezolid is the first approved oxazolidinone antibacterial agent, whereas PH027 is a novel compound of the same class that exhibits good in vitro antibacterial activity. The objective of this study was to develop an UPLC-MS/MS assay for the analysis of linezolid and PH027 in plasma and to apply the method for comparative pharmacokinetic and tissue distribution studies of both compounds. METHOD: Plasma samples and calibrators were extracted with diethyl ether after addition of the internal standard solution...
January 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27959474/cyanuric-acid-based-organocatalyst-for-utilization-of-carbon-dioxide-at-atmospheric-pressure
#10
Bing Yu, Daeun Kim, Seoksun Kim, Soon Hyeok Hong
A novel and efficient organocatalytic system, based on economical and readily available cyanuric acid, was developed for the synthesis of 2-oxazolidinones and quinazoline-2,4(1H,3H)-diones from propargylamines and 2-aminobenzonitriles under atmospheric pressure carbon dioxide. Notably, a low concentration of carbon dioxide in air was directly converted into 2-oxazolidinone in excellent yields without an external base. Through mechanistic investigation including in situ FT-IR spectroscopy, cyanuric acid was demonstrated to be an efficient catalyst for carbon dioxide fixation...
December 13, 2016: ChemSusChem
https://www.readbyqxmd.com/read/27941424/characterization-of-neurologic-and-ophthalmologic-safety-of-oral-administration-of-tedizolid-for-up-to-21-days-in-healthy-volunteers
#11
Edward Fang, Kelly A Muñoz, Philippe Prokocimer
BACKGROUND: Antibacterials that inhibit protein synthesis may be associated with mitochondrial toxicity, manifested as serious optic or peripheral neuropathy or myelosuppression. Tedizolid is a novel oxazolidinone antibacterial that may have reduced the potential for mitochondrial toxicity. STUDY QUESTION: Based on the results of 2 studies (NCT01623401 and NCT00671814) conducted early in the tedizolid development program, what is the potential for drug-induced optic and peripheral neuropathies with tedizolid treatment? METHODS: Two phase-1 studies were conducted in healthy volunteers...
November 15, 2016: American Journal of Therapeutics
https://www.readbyqxmd.com/read/27934357/access-to-4-oxazolidinones-a-3-2-cycloaddition-approach
#12
Arjun Acharya, Karissa Montes, Christopher S Jeffrey
The novel reactivity of in situ generated aza-oxyallyl cation intermediates with a variety of carbonyl compounds is reported to construct 4-oxazolidinones motifs with good yields and diastereoselectivities. This simple and efficient (3 + 2) cycloaddition method provides direct access to potential bioactive compounds.
December 2, 2016: Organic Letters
https://www.readbyqxmd.com/read/27904526/new-agents-approved-for-treatment-of-acute-staphylococcal-skin-infections
#13
Jan Tatarkiewicz, Anna Staniszewska, Magdalena Bujalska-Zadrożny
Vancomycin has been a predominant treatment for methicillin-resistant Staphylococcus aureus (MRSA) infections for decades. However, growing reservations about its efficacy led to an urgent need for new antibiotics effective against MRSA and other drug-resistant Staphylococcus aureus strains. This review covers three new anti-MRSA antibiotics that have been recently approved by the FDA: dalbavancin, oritavancin, and tedizolid. The mechanism of action, indications, antibacterial activity profile, microbial resistance, pharmacokinetics, clinical efficacy, adverse effects, interactions as well as available formulations and administration of each of these new antibiotics are described...
December 1, 2016: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/27904038/a-retrospective-analysis-of-risk-factors-for-linezolid-associated-hyponatremia-in-japanese-patients
#14
Ryota Tanaka, Yosuke Suzuki, Yukie Takumi, Motoshi Iwao, Yuhki Sato, Kazuhiko Hashinaga, Kazufumi Hiramatsu, Jun-Ichi Kadota, Hiroki Itoh
Linezolid is an oxazolidinone antibiotic against Gram-positive bacteria. Although thrombocytopenia is a major adverse effect of linezolid, hyponatremia also often develops after linezolid administration. This study examined the frequency of hyponatremia that developed during linezolid treatment and identified its risk factors. In this retrospective, single-center, observational cohort study, 61 hospitalized patients treated with linezolid between January 2013 and January 2015 were analyzed. Hyponatremia was defined as a sodium level of ≤134 mEq/L for the duration of linezolid treatment...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27891339/bacteriological-profile-of-isolates-from-urine-samples-in-patients-of-benign-prostatic-hyperplasia-and-or-prostatitis-showing-lower-urinary-tract-symptoms
#15
Prem Prakash Mishra, Ved Prakash, Kashmir Singh, H Mog, Sumit Agarwal
INTRODUCTION: The incidence of Benign Prostatic Hyperplasia (BPH) or Prostatitis is increasing considerably worldwide. The Lower Urinary Tract Symptoms (LUTS) due to bacterial aetiology are one of the common factors for the complications among the patients. AIM: To determine the bacterial agents and their antibiotic sensitivity pattern from the urine samples of patients of BPH or Prostatitis showing symptoms of LUTS. MATERIALS AND METHODS: The cross-sectional study was carried out in the Department of Microbiology of Rohilkhand Medical College and Hospital of Northern India from June 2014 to May 2015...
October 2016: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/27860345/in%C3%A2-situ-generated-zinc-ii-catalyst-for-incorporation-of-co2-into-2-oxazolidinones-with-propargylic-amines-at-atmospheric-pressure
#16
Xi Liu, Mei-Yan Wang, Si-Yuan Wang, Qi Wang, Liang-Nian He
Incorporation of CO2 into heterocyclic compounds (i.e., 2-oxazolidinones) under mild conditions, especially at atmospheric pressure still remains challenging. The mononuclear Zn(II) complex ZnCl2 (TBD)2 , where TBD=1,5,7-triazabicyclo[4.4.0]dec-5-ene, in this study was demonstrated as a robust catalyst for the carboxylative cyclization of propargylic amines with CO2 to exclusively afford various 2-oxazolidinones in excellent yields. Notably, the Zn(II) catalytic species is readily generated in situ from ZnCl2 and TBD without pre-preparation and further isolation...
November 8, 2016: ChemSusChem
https://www.readbyqxmd.com/read/27771947/rapid-and-sensitive-detection-of-3-amino-2-oxazolidinone-using-a-quantum-dot-based-immunochromatographic-fluorescent-biosensor
#17
Tao Le, Yong Xie, Liqian Zhu, Lei Zhang
To monitor the levels of furazolidone in edible animal tissues, a fluorescent sensor was developed for the determination of 3-amino-2-oxazolidinone (AOZ), the metabolite of furazolidone, featuring an immunochromatographic test strip assay (ITSA) integrated with a quantum dot (QD) label. The optimal QD-based ITSA sensor exhibits good dynamic linear detection for AOZ over the range of 0.1-100 μg/L, with a 50% inhibitory concentration (IC50) of 1.06 μg/L. The decision limit and the detection capability were 0...
November 16, 2016: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/27767302/condensation-of-carboxylic-acids-with-non-nucleophilic-n-heterocycles-and-anilides-using-boc2o
#18
Atsushi Umehara, Hirofumi Ueda, Hidetoshi Tokuyama
A novel condensation reaction of carboxylic acids with various non-nucleophilic N-heterocycles and anilides was developed. The reaction proceeds in the presence of di-tert-butyl dicarbonate (Boc2O), catalytic 4-(dimethylamino)pyridine (DMAP), and 2,6-lutidine and is applicable to the acylation of a wide range of non-nucleophilic nitrogen compounds, including indoles, pyrroles, pyrazole, carbazole, lactams, oxazolidinones, and anilides with high functional group compatibility. The scope of indoles, carboxylic acids, and anilides was also studied...
November 18, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27753442/an-medt-study-of-the-carbenoid-type-3-2-cycloaddition-reactions-of-nitrile-ylides-with-electron-deficient-chiral-oxazolidinones
#19
Luis R Domingo, Mar Ríos-Gutiérrez, Patricia Pérez
The molecular mechanism of the carbenoid-type [3 + 2] cycloaddition (32CA) reactions of a nitrile ylide (NY) with a non-chiral and a chiral oxazolidinone has been studied within Molecular Electron Density Theory (MEDT) at the MPWB1K/6-31G(d) computational level. Topological analysis of the Electron Localisation Function (ELF) of the NY shows that it presents a carbenoid structure. The high nucleophilic character of the NY together with the electrophilic character of the non-chiral oxazolidinone favour a polar 32CA reaction with a very low activation energy, the reaction being completely meta/endo selective...
October 18, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27748168/occurrence-and-levels-of-nitrofuran-metabolites-in-sea-cucumber-from-dalian-china
#20
Hongxia Zhao, Wuxia Guo, Wenna Quan, Jingqiu Jiang, Baocheng Qu
The occurrence and levels of nitrofuran metabolites (NFMs) in sea cucumber (SC) from Dalian, China, are reported. Four metabolites including 3-amino-5-morpholinomethyl-2-oxazolidinone (AMOZ), 3-amino-2-oxazolidinone (AOZ), semicarbazide (SEM) and 1-aminohydantoin (AHD) in different SC products (fresh, instant and dry salted SCs) were measured. The frequency of occurrence for NFMs in all SC samples was 42.7%. The total NFM concentrations ranged from non-detectable to 64.6 ng g(-)(1), with a mean of 3.59 ng g(-1)...
November 2016: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
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