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Pan-Lin Shao, Zi-Rui Li, Zhi-Peng Wang, Ming-Hui Zhou, Qi Wu, Ping Hu, Yun He
The first formal [3 + 2] cycloaddition reaction of in situ-generated azaoxyallyl cation with cyclic ketones has been developed using mild reaction conditions. A variety of spiro-4-oxazolidinones was obtained in excellent yields (up to 99%). The high efficiency of this process, coupled with the operational simplicity, makes it an attractive method for the synthesis of spiro-4-oxazolidinones.
September 19, 2017: Journal of Organic Chemistry
Mahtab Beitdaghar, Roya Ahmadrajabi, Afsaneh Karmostaji, Fereshteh Saffari
BACKGROUND: The increasing incidence of antimicrobial resistance has led to research on finding new antimicrobial agents or identifying drug combinations with synergistic effects. Enterococcal infections, particularly those associated with vancomycin-resistant enterococci (VREs), are therapeutic problems. Linezolid (LZD), an oxazolidinone antibiotic, shows good activity against Gram-positive bacteria including enterococci. To avoid the emergence of linezolid-resistant subpopulations and achieve enhanced activity or bactericidal effect, the use of combined therapy has been considered...
September 18, 2017: Wiener Medizinische Wochenschrift
Barbara A Brown-Elliott, Richard J Wallace
There is a paucity of efficacious antimicrobials (especially oral) against clinically relevant species of Nocardia To date, all species of Nocardia have been susceptible to linezolid, the first commercially available oxazolidinone. Tedizolid is a new oxazolidinone with previously reported improved in vitro and in vivo (intracellular) potency against multidrug resistant strains of Mycobacterium sp., and Nocardia brasiliensis Using the current Clinical and Laboratory Standards Institute recommended broth microdilution method, 101 isolates of Nocardia spp, including 29 N...
September 18, 2017: Antimicrobial Agents and Chemotherapy
Pauline Ract, Caroline Piau-Couapel, Fabrice Compain, Michel Auzou, Jocelyn Michon, Vincent Cattoir
Tedizolid, a second-generation oxazolidinone that displays a potent activity against Gram-positive pathogens, could be an interesting option for the treatment of bone and joint infections (BJIs). The aim of the study was to determine minimal inhibitory concentration (MIC) of tedizolid against a collection of 359 clinical isolates involved in clinically-documented BJIs and to compare them to those of comparator agents used in Gram-positive infections. Of the 104 Staphylococcus aureus and 102 coagulase-negative staphylococci (CoNS) isolates, 99 and 92 % were categorized as susceptible to tedizolid, respectively (MIC25=0...
September 18, 2017: Journal of Medical Microbiology
Qian Tang, Yanfang Zhao, Boxuan Xu, Ping Gong, Di Wang
 Oxazolidinones comprise a novel class of antimicrobials as inhibitors of bacterial ribosomal protein synthesis. In the present study, we identified 15 novel oxazolidinone analogues with potent antituberculosis activities. Compounds sy124 and sy125 displayed the best antituberculosis activity in vitro, against various clinically relevant bacterial species, including most Gram positive bacteria, Mycobacterium and Helicobacter pylori, which are better than that of the linezolid. Cell based assay indicated that these compounds showed strong ability to kill the intracellular pathogens...
September 11, 2017: Japanese Journal of Infectious Diseases
Gaopeng Song, Xiang Zhu, Junhua Li, Dekun Hu, Dongsheng Zhao, Yixian Liao, Juntong Lin, Lian-Hui Zhang, Zi-Ning Cui
Improvement of subtype selectivity of an inhibitor's binding activity using the conformational restriction approach has become an effective strategy in drug discovery. In this study, we applied this approach to PDE4 inhibitors and designed a series of novel oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as conformationally restricted analogues of rolipram. The bioassay results demonstrated the oxazolidinone-fused tetrahydroisoquinoline derivatives exhibited moderate to good inhibitory activity against PDE4B and high selectivity for PDE4B/PDE4D...
September 1, 2017: Bioorganic & Medicinal Chemistry
Gianluca Morroni, Andrea Brenciani, Serena Simoni, Carla Vignaroli, Marina Mingoia, Eleonora Giovanetti
No abstract text is available yet for this article.
2017: Frontiers in Microbiology
Mohsen A Hedaya, Vidhya Thomas, Mohamed E Abdel-Hamid, Elijah O Kehinde, Oludotun A Phillips
This is a comparative pharmacokinetics study of linezolid (Lzd), and two novel oxazolidinone antibacterial agents-PH027 and PH051-in rabbits to determine if the discrepancy between the in vitro and in vivo activities of the novel compounds is due to pharmacokinetic factors. The pharmacokinetics after IV and oral administration, plasma protein binding and tissue distribution for the three compounds were compared. The elimination half-lives were 52.4 ± 6.3, 68.7 ± 12.1 and 175 ± 46.1 min for Lzd, PH027 and PH051, respectively...
September 7, 2017: Pharmaceutics
David Lupton, Matthew J Belousoff
No abstract text is available yet for this article.
September 6, 2017: Future Microbiology
Sarah E Hobdey, Eva J Katahira, Pamela Dockstader, Stephen M Davidson, Laura Bond, Devin D Bolz, Amy E Bryant, Dennis L Stevens
This study investigates the effects of subinhibitory doses of the second-generation lipoglycopeptide antibiotic, dalbavancin, on Staphylococcus aureus toxin production in vitroS. aureus toxin production was compared with the natural glycopeptide antibiotic, vancomycin, and representative beta-lactam and oxazolidinone antibiotics. While neither dalbavancin nor vancomycin adversely increased toxin production, of these glycopeptide antibiotics, only dalbavancin significantly attenuated toxin production as subinhibitory concentrations...
September 5, 2017: Antimicrobial Agents and Chemotherapy
Izabela Karpiuk, Stefan Tyski
This paper is the fifth part of the series concerning the search for new preparations for antibacterial therapy and discussing new compounds belonging to the oxazolidinone class of antibacterial chemotherapeutics. This article presents five new substances that are currently at the stage of clinical trials (radezolid, sutezolid, posizolid, LCB01-0371 and MRX-I). The intensive search for new antibiotics and antibacterial chemotherapeutics with effective antibacterial activity is aimed at overcoming the existing resistance mechanisms in order to effectively fight against multidrug-resistant bacteria, which pose a real threat to public health...
2017: Przegla̧d Epidemiologiczny
Yun Kim, Anhye Kim, SeungHwan Lee, Sung-Hak Choi, Dae Young Lee, Ji-Su Song, Howard Lee, In-Jin Jang, Kyung-Sang Yu
PURPOSE: Tedizolid phosphate is a next-generation oxazolidinone prodrug that is transformed into the active moiety tedizolid. Its indication is acute bacterial skin and skin structure infections caused by gram-positive species, including methicillin-resistant Staphylococcus aureus. Although tedizolid phosphate has been marketed in Korea, no data on the pharmacokinetic (PK) properties or tolerability of tedizolid phosphate in Korean subjects are available. This study was designed to evaluate the PK properties, oral bioavailability, and tolerability with a single-dose oral and intravenous administration of tedizolid phosphate in healthy Korean male subjects...
August 30, 2017: Clinical Therapeutics
Romain Rey-Rodriguez, Gwendal Grelier, Loïc Habert, Pascal Retailleau, Benjamin Darses, Isabelle Gillaizeau, Philippe Dauban
This article describes the reaction of ynamides with metallanitrenes generated in the presence of an iodine(III) oxidant. N-(Boc)-Ynamides are converted to oxazolones via a cyclization reaction. The reaction is mediated by a catalytic dirhodium-bound nitrene species that first behaves as a Lewis acid. The oxazolones can be converted in a one pot manner to functionalized oxazolidinones following a regio- and stereoselective oxyamination reaction with the same nitrene reagent generated in stoichiometric amounts...
September 1, 2017: Journal of Organic Chemistry
Jian Liang Low, Mu-Lu Wu, Dinah Binte Aziz, Benoît Laleu, Thomas Dick
The prevalence of lung disease due to infections with nontuberculous mycobacteria (NTM) has been increasing and surpassed tuberculosis (TB) in some countries. Treatment outcomes are often unsatisfactory, highlighting an urgent need for new anti-NTM medications. Although NTM in general do not respond well to TB specific drugs, the similarities between NTM and Mycobacterium tuberculosis at the molecular and cell structural level suggest that compound libraries active against TB could be leveraged for NTM drug discovery...
2017: Frontiers in Microbiology
Subhadip De, Junli Yin, Dawei Ma
Cu2O/N,N'-bis(thiophen-2-ylmethyl)oxalamide is established to be an effective catalyst system for Goldberg amidation with inferior reactive (hetero)aryl chlorides, which have not been efficiently documented by Cu-catalysis to date. The reaction is well liberalized toward a variety of functionalized (hetero)aryl chlorides and a wide range of aromatic and aliphatic primary amides in good to excellent yields. Furthermore, the arylation of lactams and oxazolidinones is achieved. The present catalytic system also accomplished an intramolecular cross-coupling product...
August 31, 2017: Organic Letters
James A Karlowsky, Meredith A Hackel, Samuel K Bouchillon, Jeff Alder, Daniel F Sahm
Clinical isolates of Staphylococcus aureus (n=3929) collected by 54 medical center laboratories in 12 countries in 2014-2016 were tested for in vitro susceptibility to tedizolid, linezolid, and 11 comparators using Clinical and Laboratory Standards Institute (CLSI) broth microdilution methodology with minimum inhibitory concentrations (MICs) interpreted by CLSI M100-S26 (2016) criteria. All isolates of S. aureus tested were susceptible to both tedizolid (MIC, ≤0.5μg/mL) and linezolid (MIC, ≤4μg/mL). The concentration of tedizolid that inhibited 90% of isolates (MIC90) was 0...
July 8, 2017: Diagnostic Microbiology and Infectious Disease
Carlos Heras, Alejandro Gómez-Palomino, Pedro Romea, Fèlix Urpí, Josep Maria Bofill, Ibério de P R Moreira
Quantum chemical calculations have unveiled the unexpected biradical character of titanium(IV) enolates from N-acyl oxazolidinones and thiazolidinethiones. The electronic structure of these species therefore involves a valence tautomerism consisting of an equilibrium between a closed shell (formally Ti(IV) enolates) and an open shell, biradical, singlet (formally Ti(III) enolates) electronic states, whose origin is to be basically found in changes of the Ti-O distance. Spectroscopic studies of the intermediate species lend support to such a model, which also turns out to be crucial for a better understanding of the overall reactivity of titanium(IV) enolates...
August 21, 2017: Journal of Organic Chemistry
Matthew B McNeil, Devon Dennison, Catherine Shelton, Tanya Parish
Oxazolidinones are promising candidates for the treatment of Mycobacterium tuberculosis infections. We isolated linezolid resistant strains from H37Rv (Euro-American) and HN878 (East-Asian) strains; resistance frequency was similar in both strains. Mutations were identified in ribosomal protein L3 (RplC) and the 23S rRNA (rrl). All mutant strains were cross resistant to sutezolid; a subset were cross-resistant to chloramphenicol. Mutations in rrl led to growth impairment and decreased fitness that could limit spread in clinical settings...
July 31, 2017: Antimicrobial Agents and Chemotherapy
Abdullah Alsultan, Jennifer J Furin, Jeannine Du Bois, Elana van Brakel, Phalkun Chheng, Amour Venter, Bonnie Thiel, Sara A Debanne, W Henry Boom, Andreas H Diacon, John L Johnson, Charles A Peloquin
AZD-5847 is a new oxazolidinone derivative under development for the treatment of tuberculosis. In this study we describe the population pharmacokinetics of AZD-5847 in patients with tuberculosis based on a recently completed phase II study. The study included 60 patients with drug susceptible TB. Patients were randomized to four doses (500 mg once daily, 1200 mg once daily, 500 mg twice daily and 800 mg twice daily). Patients were intensively sampled on day 1 and 14. AZD-5847 pharmacokinetics were best described with a two compartment system with tlag for absorption...
July 24, 2017: Antimicrobial Agents and Chemotherapy
Hamidreza Houri, Hossein Kazemian, Hadi Sedigh Ebrahim-Saraie, Asieh Taji, Zahra Tayebi, Hamid Heidari
OBJECTIVES: The aim of the study was to investigate the linezolid activity against clinical Gram-positive cocci with advanced antimicrobial drug resistance. METHODS: A collection of methicillin resistant Staphylococcus aureus (MRSA), vancomycin resistant enterococci (VRE), penicillin non-susceptible Streptococcus pneumoniae (PNSP), and group B streptococci (GBS) were isolated from various clinical samples. Antimicrobial susceptibility tests were done using standard methods Subsequently, we investigated linezolid antibacterial activities, the first approved oxazolidinone against isolates by the standard broth microdilution method...
September 2017: Journal of Global Antimicrobial Resistance
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