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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
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
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
Xi Liu, Mei-Yan Wang, Si-Yuan Wang, Qi Wang, Liang-Nian He
Incorporation of CO2 into heterocycle compounds i.e. 2-oxazolidinones under mild conditions, especially at atmospheric pressure still remains challenging. The mononuclear zinc(II) complex viz. ZnCl2(TBD)2 in this study was for the first time 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 zinc(II) catalytic species is readily in situ generated from zinc dichloride and 1,5,7-triazabicyclo[4...
November 8, 2016: ChemSusChem
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 3, 2016: Journal of Agricultural and Food Chemistry
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 1, 2016: Journal of Organic Chemistry
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
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)...
October 17, 2016: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
Rosario Musumeci, Enrico Calaresu, Jolanda Gerosa, Davide Oggioni, Simone Bramati, Patrizia Morelli, Ida Mura, Andrea Piana, Bianca Maria Are, Clementina Elvezia Cocuzza
Linezolid is the main representative of the oxazolidinones, introduced in 2000 in clinical practice to treat severe Gram-positive infections. This compound inhibits protein synthesis by binding to the peptidyl transferase centre of the 50S bacterial ribosomal subunit. The aim of this study was to characterize 12 clinical strains of linezolid-resistant Staphylococcus spp. isolated in Northern Italy. All isolates of Staphylococcus spp. studied showed a multi-antibiotic resistance phenotype. In particular, all isolates showed the presence of the mecA gene associated with SSCmec types IVa, V or I...
September 13, 2016: New Microbiologica
Rustam Aminov
The introduction of antibiotics into clinical practice revolutionized the treatment and management of infectious diseases. Before the introduction of antibiotics, these diseases were the leading cause of morbidity and mortality in human populations. This review presents a brief history of discovery of the main antimicrobial classes (arsphenamines, β-lactams, sulphonamides, polypeptides, aminoglycosides, tetracyclines, amphenicols, lipopeptides, macrolides, oxazolidinones, glycopeptides, streptogramins, ansamycins, quinolones, and lincosamides) that have changed the landscape of contemporary medicine...
October 5, 2016: Biochemical Pharmacology
Jingdong Shi, Ying Jiang, Yanfang Zhao
The objective of this study was to investigate the prevalence of drug-resistant Helicobacter pylori in Beijing Tian Tan Hospital (Beijing, China) and to determine the susceptibility of H. pylori to linezolid and novel oxazolidinone analogues. Minimum inhibitory concentrations (MICs) of amoxicillin, clarithromycin, metronidazole, ciprofloxacin, tetracycline and levofloxacin against H. pylori were determined by Etest. The in vitro antibacterial activities of linezolid and novel oxazolidinone analogues were assessed by the disk diffusion method...
December 2016: Journal of Global Antimicrobial Resistance
Rosa Padilla, Verónica Salazar-Pereda, Daniel Mendoza-Espinosa, José M Vásquez-Pérez, Noemí Andrade-López, Joaquín Tamariz, José G Alvarado-Rodríguez, Julián Cruz-Borbolla
The Ir(i) complexes [Tp(Me2)Ir(η(4)-1,4-diene)] 2b and 2c react thermally with a variety of aromatic aldehydes, 3a-e, to generate the metallabicyclic compounds 4e-k and the Fischer-type carbenes 5a-b in moderate yields. These reactions are proposed to take place with the initial formation of η(1)-aldehyde adducts as key intermediates. The formation of the metallabicyclic compounds 4e-k involves a formal decarboxylation process at the exo-2-oxazolidinone diene and an ortho metallation of the aromatic ring...
September 29, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Zhoujie Luo, Binsen Wang, Yuan Liu, Guohua Gao, Fei Xia
The mechanisms of the one-pot conversion of carbon dioxide, ethylene oxide, and aniline to 3-phenyl-2-oxazolidionone catalyzed by the binary ionic liquids of BmimBr and BmimOAc were explored using the DFT methods. The complex reaction above comprises of two parallel reactions and a subsequent cascade reaction. DFT calculations on reaction pathways and energy profiles reveal that the electrostatic and hydrogen-bond effects of BmimBr play a crucial role in the parallel reactions for the generation of ethylene carbonate and 2-phenylamino-ethanol...
October 12, 2016: Physical Chemistry Chemical Physics: PCCP
D J Biedenbach, S K Bouchillon, B Johnson, J Alder, D F Sahm
Tedizolid is an oxazolidinone with an antimicrobial in vitro potency advantage against Gram-positive bacterial pathogens compared to other currently marketed drugs in this class, including linezolid. Tedizolid was compared to linezolid when tested against Staphylococcus aureus and Streptococcus pneumoniae isolates collected from countries in Latin America and the Asia-Pacific. Isolates were tested by broth microdilution susceptibility methods against tedizolid, linezolid, and non-class comparators in accordance with the Clinical and Laboratory Standards Institute (CLSI) guidelines...
December 2016: European Journal of Clinical Microbiology & Infectious Diseases
Lucia Ferrazzano, Angelo Viola, Elena Lonati, Alessandra Bulbarelli, Rosario Musumeci, Clementina Cocuzza, Marco Lombardo, Alessandra Tolomelli
Among the different classes of antibiotics, oxazolidinone derivatives represent important drugs, since their unique mechanism of action overcomes commonly diffused multidrug-resistant bacteria. Anyway, the structural similarity of these molecules to monoamino oxidase (MAO) inhibitors, like toloxatone and blefoxatone, induces in many cases loss of selectivity as a major concern. A small library of compounds based on isoxazolidinone and dehydro-β-proline scaffold was designed with the aim to obtain antibacterial agents, evaluating at the same time the potential effects of structural features on MAO inhibitory behaviour...
September 4, 2016: European Journal of Medicinal Chemistry
Run Fan, Dexi Li, Yang Wang, Tao He, Andrea T Feßler, Stefan Schwarz, Congming Wu
A total of 57 methicillin-resistant Staphylococcus aureus (MRSA) isolates and 475 methicillin-resistant coagulase-negative staphylococci (MRCoNS) collected from pigs in the Guangdong province of China in 2014 were investigated for the presence of the novel oxazolidinone-phenicol resistance gene optrA The optrA gene was detected in 6.9% (n = 33) of the MRCoNS, all of which were Staphylococcus sciuri isolates, but in none of the MRSA isolates. Five optrA-carrying methicillin-resistant (MR) S. sciuri isolates also harbored the multiresistance gene cfr Pulsed-field gel electrophoresis (PFGE) and dru typing of the 33 optrA-carrying MR S...
December 2016: Antimicrobial Agents and Chemotherapy
Tarani Kanta Barman, Manoj Kumar, Tarun Mathur, Tridib Chaira, G Ramkumar, Vandana Kalia, Madhvi Rao, Manisha Pandya, Ajay Singh Yadav, Biswajit Das, Dilip J Upadhyay, Hamidullah, Rituraj Konwar, V Samuel Raj, Harpal Singh
RBx 11760, a bi-aryl oxazolidinone, was investigated for antibacterial activity against Gram-positive bacteria. The MIC90s of RBx 11760 and linezolid against Staphylococcus aureus were 2 and 4 mg/liter, against Staphylococcus epidermidis were 0.5 and 2 mg/liter, and against Enterococcus were 1 and 4 mg/liter, respectively. Similarly, against Streptococcus pneumoniae the MIC90s of RBx 11760 and linezolid were 0.5 and 2 mg/liter, respectively. In time-kill studies, RBx 11760, tedizolid, and linezolid exhibited bacteriostatic effect against all tested strains except S...
December 2016: Antimicrobial Agents and Chemotherapy
Lanqing Cui, Yang Wang, Yuan Lv, Shan Wang, Yunjia Song, Yun Li, Jian Liu, Feng Xue, Weiwei Yang, Jia Zhang
A total of 2,201 nonduplicate enterococcal isolates collected from 29 hospitals in 23 cities in China between 2004 and 2014 were screened for the oxazolidinone resistance gene optrA; 45 isolates (2.0%) were optrA positive with 11 OptrA variants identified. The positive rate of optrA increased from 0.4% to 3.9% during the 10-year surveillance period. Pulsed-field gel electrophoresis (PFGE) and multilocus sequence type (MLST) analysis revealed that 37 optrA-positive Enterococcus faecalis isolates clustered into 25 PFGE patterns and 21 sequence types, while 6 Enterococcus faecium isolates represented 6 PFGE patterns and 6 sequence types...
December 2016: Antimicrobial Agents and Chemotherapy
Wenqing Hu, Bing Shi, Lihui Liu, Shengke He, Liping Ye, DengMei Tian, Yongqing Zhang
Linezolid (LZD), severed as the first oxazolidinone antibiotic, was active against multidrug-resistant gram-positive strains. LZD can induce thrombocytopenia, anemia and leukocytopenia. Currently, reports on pure red cell aplasia (PRCA) cases induced by LZD are relatively rare (4-7). In this paper, we reported a patient with PRCA twice induced by LZD. A 37-year-old man was diagnosed with myelodysplatic syndrome (MDS) and underwent allo-HSCT from an unrelated donor with ABO blood type and leukocyte antigen (HLA)-matching...
2016: Iranian Journal of Pharmaceutical Research: IJPR
Khuloud Takrouri, Harold D Cooper, Andrew Spaulding, Paola Zucchi, Bilyana Koleva, Dillon C Cleary, Westley Tear, Penny J Beuning, Elizabeth B Hirsch, James B Aggen
Novel antibacterials with activity against the Gram-negative bacteria associated with nosocomial infections, including Escherichia coli and other Enterobacteriaceae, are urgently needed due to the increasing prevalence of multidrug-resistant strains. A major obstacle that has stalled progress on nearly all small-molecule classes with potential for activity against these species has been achieving sufficient whole-cell activity, a difficult challenge due to the formidable outer membrane and efflux barriers intrinsic to these species...
June 10, 2016: ACS Infectious Diseases
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