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oxazolidinone

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https://www.readbyqxmd.com/read/29751119/bacteriological-relevance-of-linezolid-versus-vancomycin-in-postoperative-empirical-treatment-of-osteoarticular-infections-a-retrospective-single-center-study
#1
E Takoudju, P Bemer, S Touchais, N Asseray, S Corvec, L Khatchatourian, N Serandour, D Boutoille
BACKGROUND: Our center replaced vancomycin by linezolid in 2015 for the postoperative empirical treatment of osteoarticular infections (OAI). OBJECTIVES: This work aims to assess the bacteriological relevance of linezolid for orthopaedic postoperative probabilistic antibiotic therapy. METHODS: Analysis of an observational cohort of patients empirically treated by a combination of linezolid with piperacillin/tazobactam during the immediate postoperative stage for an OAI between July 1st 2015 and July 1st 2016, in a French reference center...
May 8, 2018: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/29739573/highly-sensitive-furazolidone-monitoring-in-milk-by-a-signal-amplified-lateral-flow-assay-based-on-magnetite-nanoparticles-labeled-dual-probe
#2
Lingzhi Yan, Leina Dou, Tong Bu, Qiong Huang, Rong Wang, Qingfeng Yang, Lunjie Huang, Jianlong Wang, Daohong Zhang
We presented a signal amplified lateral flow assay (LFA) based on magnetite nanoparticles (MNPs) labeled dual-probe and applied it in the high sensitive and rapid on-site detection of furazolidone metabolite of 3-amino-2-oxazolidinone (AOZ). The amplified signal benefited from high affinity between two probes of MNPs labeled murine monoclonal antibody (MNPs-MAb) and goat anti-mouse antibody (MNPs-GAMA) and was achieved by the generation of dual-probe network complex. This developed method could realize high sensitive detection of AOZ with a threshold value of 0...
September 30, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29733362/in-vitro-induced-erythromycin-resistance-facilitates-cross-resistance-to-the-novel-fluoroketolide-solithromycin-in-staphylococcus-aureus
#3
Weiming Yao, Guangjian Xu, Bing Bai, Hongyan Wang, Minggui Deng, Jinxin Zheng, Duoyun Li, Xiangbin Deng, Xiaojun Liu, Zhiwei Lin, Zhong Chen, Guiqiu Li, Qiwen Deng, Zhijian Yu
The aim of this study was to determine whether in vitro induced erythromycin resistance facilitates the cross-resistance to the novel fluoroketolide, solithromycin, in Staphylococcus aureus. Four strains of methicillin-susceptible S. aureus strains S2, S3, S5, S7 were successfully induced to establish erythromycin-resistant strains by continuous in vitro culture with erythromycin. Mutations at drug binding sites were shown to increase the minimal inhibitory concentrations for ketolides, including telithromycin and the novel compound solithromycin, but did not increase for lincosamides, chloramphenicols, or oxazolidinones...
May 3, 2018: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/29717611/oxy-alkylation-of-allylamines-with-unactivated-alkyl-bromides-and-co-2-via-visible-light-driven-palladium-catalysis
#4
Liang Sun, Jian-Heng Ye, Wen-Jun Zhou, Xin Zeng, Da-Gang Yu
A selective oxy-alkylation of allylamines with unactivated alkyl bromides and CO2 via visible-light-driven palladium catalysis is reported. The commercially available Pd(PPh3 )4 is used as the sole catalyst in this three-component reaction. A variety of tertiary, secondary, and primary alkyl bromides undergo reactions to generate important 2-oxazolidinones in high yields and selectivity. The mild reaction conditions, easy scalability, and facile derivatization of products provide great potential for application in organic synthesis and pharmaceutical chemistry...
May 2, 2018: Organic Letters
https://www.readbyqxmd.com/read/29712654/pharmacokinetics-pharmacodynamics-and-tolerability-of-single-dose-oral-lcb01-0371-a-novel-oxazolidinone-with-broad-spectrum-activity-in-healthy-volunteers
#5
Yong-Soon Cho, Hyeong-Seok Lim, Shi-Hyang Lee, Young Lag Cho, Hee-Sook Nam, Kyun-Seop Bae
LCB01-0371 is a novel oxazolidinone with broad-spectrum activity against Gram-positive pathogens in both in vitro studies and animal infection models. The objectives of this study were to evaluate its safety, tolerability, pharmacokinetics, and pharmacodynamics following single ascending doses (NCT01554995). Single oral doses of 600 mg Linezolid, a placebo, or LCB01-0371 between 50 mg and 3200 mg were tested in 69 healthy male subjects. Blood and urine were sampled, and LCB01-0371 concentrations were measured, and the serum inhibitory and bactericidal titers of LCB01-0371 and Linezolid were determined...
April 30, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29697133/influence-of-the-catalyst-structure-in-the-cycloaddition-of-isocyanates-to-oxiranes-promoted-by-tetraarylstibonium-cations
#6
Mengxi Yang, Nilanjana Pati, Guillaume Bélanger-Chabot, Masato Hirai, François P Gabbaï
In the context of our work on electron deficient group 15 cations as Lewis acid catalysts, we have synthesized the triflate salts of a series of tetraarylstibonium cations of general formula [ArSbPh3]+ with Ar = Mes (4+), o-(dimethylamino)phenyl (5+), and o-((dimethylamino)methyl)phenyl (6+). These new cationic antimony derivatives, along with the known [Ph4Sb]+ (1+), 1-naphthyltriphenylstibonium (2+), and [(Ant)SbPh3]+ (3+), have been evaluated as catalysts for the cycloaddition of oxiranes and isocyanates under mild conditions...
April 26, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29697101/selective-aqueous-acetylation-controls-the-photoanomerization-of-%C3%AE-cytidine-5-phosphate
#7
Christian Fernández-García, Natalie M Grefenstette, Matthew W Powner
Nucleic acids are central to information transfer and replication in living systems, providing the molecular foundations of Darwinian evolution. Here we report that prebiotic acetylation of the non-natural, but prebiotically plausible, ribonucleotide α-cytidine-5'-phosphate, selectively protects the vicinal diol moiety. Vicinal diol acetylation blocks oxazolidinone formation and prevents C2'-epimerization upon irradiation with UV-light. Consequently, acetylation enhances (4-fold) the photoanomerization of α-cytidine-5'-phosphate to produce the natural β-pyrimidine ribonucleotide-5'-phosphates required for RNA synthesis...
April 26, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29659858/zaaps-programme-results-for-2016-an-activity-and-spectrum-analysis-of-linezolid-using-clinical-isolates-from-medical-centres-in-42-countries
#8
Rodrigo E Mendes, Lalitagauri Deshpande, Jennifer M Streit, Helio S Sader, Mariana Castanheira, Patricia A Hogan, Robert K Flamm
Objectives: To report the linezolid activity, resistance mechanisms and epidemiological typing of selected isolates observed during the 2016 Zyvox® Annual Appraisal of Potency and Spectrum (ZAAPS) programme. Methods: A total of 8325 organisms were consecutively collected from 76 centres in 42 countries (excluding the USA). Broth microdilution susceptibility testing was performed and isolates displaying linezolid MICs of ≥4 mg/L were molecularly characterized...
April 6, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29658022/an-alkaline-resistant-ag-i-anchored-pyrazolate-based-metal-organic-framework-for-chemical-fixation-of-co-2
#9
Huimin Yang, Xu Zhang, Guiyang Zhang, Honghan Fei
An alkaline-resistant Ag(i)-anchored metal-organic framework has been achieved via postsynthetic modification of pyrazolate-based linkers. For the first time, the resultant MOF was completely heterogeneous and recyclable over at least ten cycles in cyclic carboxylation of propargyl amines and CO2 into oxazolidinones and tetramic acids under atmospheric pressure of CO2.
April 16, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29617143/oxazolidinone-mediated-sequence-determination-of-one-bead-one-compound-cyclic-peptide-libraries
#10
Hader E Elashal, Ryan D Cohen, Heidi E Elashal, Monika Raj
A novel one-bead one-compound (OBOC) dual ring-opening/cleavage approach for cyclic peptide sequencing was developed. The method selectively modifies serine, cysteine, threonine, and/or glutamic acid to an oxazolidinone-derived moiety, thereby increasing the susceptibility of the modified peptide backbone toward hydrolysis. The resulting linear peptide was then sequenced in 1 min by tandem mass spectrometry on a quadrupole time-of-flight instrument incorporating two-dimensional liquid chromatography and ion mobility spectrometry separation...
April 4, 2018: Organic Letters
https://www.readbyqxmd.com/read/29603634/current-status-of-o-heterocycles-a-synthetic-and-medicinal-overview
#11
Pankaj Kumar Singh, Om Silakari
O-heterocycles have been explored since long in the field of medicinal chemistry but they have not yet been given their due significance and are usually shunned out in comparison to N-heterocycles. Designing of bioactive molecules for almost every pathophysiological condition is primarily focused on designing novel N-heterocycles. The basic reasons for this bias are the ease of synthesis and possible mimicking of physiological molecules by N-heterocycles. But considering only this criteria never provides any breakthrough molecule for any disease condition, rather risk of toxicity/side effects are increased with such molecules...
March 30, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29584861/linezolid-pharmacokinetics-in-mdr-tb-a-systematic-review-meta-analysis-and-monte-carlo-simulation
#12
James Millard, Henry Pertinez, Laura Bonnett, Eva Maria Hodel, Véronique Dartois, John L Johnson, Maxine Caws, Simon Tiberi, Mathieu Bolhuis, Jan-Willem C Alffenaar, Geraint Davies, Derek J Sloan
Objectives: The oxazolidinone linezolid is an effective component of drug-resistant TB treatment, but its use is limited by toxicity and the optimum dose is uncertain. Current strategies are not informed by clinical pharmacokinetic (PK)/pharmacodynamic (PD) data; we aimed to address this gap. Methods: We defined linezolid PK/PD targets for efficacy (fAUC0-24:MIC >119 mg/L/h) and safety (fCmin <1.38 mg/L). We extracted individual-level linezolid PK data from existing studies on TB patients and performed meta-analysis, producing summary estimates of fAUC0-24 and fCmin for published doses...
March 23, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29581252/global-increase-and-geographic-convergence-in-antibiotic-consumption-between-2000-and-2015
#13
Eili Y Klein, Thomas P Van Boeckel, Elena M Martinez, Suraj Pant, Sumanth Gandra, Simon A Levin, Herman Goossens, Ramanan Laxminarayan
Tracking antibiotic consumption patterns over time and across countries could inform policies to optimize antibiotic prescribing and minimize antibiotic resistance, such as setting and enforcing per capita consumption targets or aiding investments in alternatives to antibiotics. In this study, we analyzed the trends and drivers of antibiotic consumption from 2000 to 2015 in 76 countries and projected total global antibiotic consumption through 2030. Between 2000 and 2015, antibiotic consumption, expressed in defined daily doses (DDD), increased 65% (21...
April 10, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29575121/manuka-honey-and-methylglyoxal-increase-the-sensitivity-of-staphylococcus-aureus-to-linezolid
#14
Gabrielle Hayes, Nicole Wright, Sarah L Gardner, Calla L Telzrow, Andrew J Wommack, Patrick A Vigueira
The continued emergence and global spread of bacterial antibiotic resistance has fueled the search for novel antimicrobial agents and resistance-modifying compounds. Manuka honey has both antimicrobial properties and the ability to increase the efficacy of FDA-approved antibiotic drugs. Compared to other types of honey, manuka honey contains elevated levels of methylglyoxal, a small molecule that contributes to its antibacterial activity. Manuka honey has shown particular promise for the treatment of antibiotic-resistant Gram-positive organisms such as methicillin-resistant Staphylococcus aureus...
March 25, 2018: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/29570872/bifunctional-squaramide-organocatalysts-for-the-asymmetric-addition-of-formaldehyde-tert-butyl-hydrazone-to-simple-aldehydes
#15
José M Lassaletta, Esteban Matador, María de Gracia Retamosa, David Monge, Javier Iglesias-Sigüenza, Rosario Fernández
The nucleophilic addition of formaldehyde tert-butyl hydrazone to simple aldehydes (a formal hetero-carbonyl-ene reaction) can be performed with good reactivities and excellent enantioselectivities by virtue of the dual H-bonding activation exerted by amide-squaramide organocatalysts. The resulting hydroxydiazenes (azo alcohols) were isolated in high yields as enantiomerically enriched azoxy compounds after a regioselective azo-to-azoxy transformation. Subsequent derivatizations provide an entry to relevant amino alcohols, oxazolidinones and derivatives thereof...
March 23, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29570624/recent-developments-in-vinylsulfonium-and-vinylsulfoxonium-salt-chemistry
#16
REVIEW
Mukulesh Mondal, Shi Chen, Nessan J Kerrigan
This review describes advances in the literature since 2000 in the area of reactions of vinylsulfonium and vinylsulfoxonium salts, with a particular emphasis on stereoselective examples. Although the chemistry of vinylsulfonium salts was first explored back in the 1950s, and that of vinylsulfoxonium salts in the early 1970s, there has been renewed interest in these compounds since the turn of the century. This has been largely due to an increased appreciation for the many synthetic possibilities associated with these valuable electrophiles...
March 23, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29566580/structural-exploration-of-hydroxyethylamines-as-hiv-1-protease-inhibitors-new-features-identified
#17
S A Amin, N Adhikari, S Bhargava, T Jha, S Gayen
The current study deals with chemometric modelling strategies (Naïve Bayes classification, hologram-based quantitative structure-activity relationship (HQSAR), comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA)) to explore the important features of hydroxylamine derivatives for exerting potent human immunodeficiency virus-1 (HIV-1) protease inhibition. Depending on the statistically validated reliable and robust quantitative structure-activity relationship (QSAR) models, important and crucial structural features have been identified that may be responsible for enhancing the activity profile of these hydroxylamine compounds...
March 23, 2018: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/29554424/a-synthetic-dual-drug-sideromycin-induces-gram-negative-bacteria-to-commit-suicide-with-a-gram-positive-antibiotic
#18
Rui Liu, Patricia A Miller, Sergei B Vakulenko, Nichole K Stewart, William C Boggess, Marvin J Miller
Many antibiotics lack activity against Gram-negative bacteria because they cannot permeate the outer membrane or suffer from efflux and, in the case of β-lactams, are degraded by β-lactamases. Herein, we describe the synthesis and studies of a dual drug conjugate (1) of a siderophore linked to a cephalosporin with an attached oxazolidinone. The cephalosporin component of 1 is rapidly hydrolyzed by purified ADC-1 β-lactamase to release the oxazolidinone. Conjugate 1 is active against clinical isolates of Acinetobacter baumannii as well as strains producing large amounts of ADC-1 β-lactamase...
March 19, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29530843/the-combination-of-tedizolid-and-daptomycin-against-methicillin-resistant-staphylococcus-aureus-in-an-in-vitro-model-of-simulated-endocardial-vegetations
#19
Jordan R Smith, Juwon Yim, Seth Rice, Kyle Stamper, Razie Kebriaei, Michael J Rybak
Background: Methicillin-resistant Staphylococcus aureus (MRSA) is a major pathogen responsible for healthcare-associated infections, and treatment options are limited. Tedizolid (TZD), is a novel, oxazolidinone antibiotic with activity against MRSA. Previously, daptomycin (DAP), has demonstrated synergy with other antibiotics against MRSA. We sought to determine the efficacy of the combination of TZD + DAP against MRSA in an in vitro model of simulated endocardial vegetations (SEVs). Methods: TZD simulations of 200 mg once daily and DAP simulations of 6-mg/kg and 10-mg/kg once daily were tested alone and in the combinations of TZD + DAP 6-mg/kg or DAP 10-mg/kg against two clinical strains of MRSA, 494 and 67...
March 12, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29525219/design-synthesis-and-biological-evaluation-of-spiropyrimidinetriones-oxazolidinone-derivatives-as-antibacterial-agents
#20
Asher M Siddiqui, Jitendra A Sattigeri, Kalim Javed, Syed Shafi, M Shamim, Smita Singhal, Zubbair M Malik
Gram-positive bacteria are among the most common human pathogens associated with clinical infections which range from mild skin infections to sepsis. Resistance towards existing class of drugs by Gram-positive bacteria including methicillin resistant Staphylococcus aureus (MRSA), Staphylococcus epidermidis (MRSE) and vancomycin resistant enterococci (VRE) is a growing concern. There is an urgent need to discover new antibiotics which are active against resistant strains of Gram positive bacteria. We report herein a novel class of spiropyrimidinetrione oxazolidinone derivatives as novel antibacterial agents...
April 15, 2018: Bioorganic & Medicinal Chemistry Letters
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