keyword
https://read.qxmd.com/read/38516805/phosphine-catalyzed-synthesis-and-cytotoxic-evaluation-of-michael-adducts-of-the-sesquiterpene-lactone-arglabin
#1
JOURNAL ARTICLE
Alexey Valeryevich Salin, Andrey A Shabanov, Khasan R Khayarov, Daut R Islamov, Alexandra D Voloshina, Syumbelya K Amerhanova, Anna P Lyubina
A general method for chemo- and diastereoselective modification of anticancer natural product arglabin with nitrogen- and carbon-centered pronucleophiles under the influence of nucleophilic phosphine catalysts was developed. The locked s-cis-geometry of α-methylene-γ-butyrolactone moiety of arglabin favors for the additional stabilization of zwitterionic intermediate by electrostatic interaction between phosphonium and enolate oxygen centers, leading to the unprecedentedly efficient phosphine-catalyzed Michael additions to this sesquiterpene lactone...
March 22, 2024: ChemMedChem
https://read.qxmd.com/read/38513340/recent-advances-in-the-exploration-of-oxazolidinone-scaffolds-from-compound-development-to-antibacterial-agents-and-other-bioactivities
#2
REVIEW
Maxwell Ampomah-Wireko, Shengcong Chen, Ruirui Li, Chen Gao, Meng Wang, Ye Qu, Hongtao Kong, Lauraine Nininahazwe, En Zhang
Bacterial infections cause a variety of life-threatening diseases, and the continuous evolution of drug-resistant bacteria poses an increasing threat to current antimicrobial regimens. Gram-positive bacteria (GPB) have a wide range of genetic capabilities that allow them to adapt to and develop resistance to practically all existing antibiotics. Oxazolidinones, a class of potent bacterial protein synthesis inhibitors with a unique mechanism of action involving inhibition of bacterial ribosomal translation, has emerged as the antibiotics of choice for the treatment of drug-resistant GPB infections...
March 13, 2024: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/38479301/identification-of-isvlu1-derived-translocatable-units-containing-optra-and-or-fexa-genes-generated-by-homologous-or-illegitimate-recombination-in-lactococcus-garvieae-of-porcine-origin
#3
JOURNAL ARTICLE
Qin Yang, Xiumei Wang, Stefan Schwarz, Yao Zhu, Wanjiang Zhang
The optrA gene encodes an ABC-F protein which confers cross-resistance to oxazolidinones and phenicols. Insertion sequence ISVlu1, a novel ISL3-family member, was recently reported to be involved in the transmission of optrA in Vagococcus lutrae. However, the role of ISVlu1 in mobilizing resistance genes has not yet fully explored. In this study, two complete and three truncated copies of ISVlu1 were found on plasmid pBN62-optrA from Lactococcus garvieae. Analysis of the genetic context showed that both optrA and the phenicols resistance gene fexA were flanked by the complete or truncated ISVlu1 copies...
March 9, 2024: Veterinary Microbiology
https://read.qxmd.com/read/38474667/optically-pure-calixarenyl-phosphine-via-stereospecific-alkylation-on-evans-oxazolidinone-moiety
#4
JOURNAL ARTICLE
Claude Bauder, David Sémeril
A convenient protocol for the synthesis of 25,26,27-tribenzoyl-28-[(( S )-1-diphenylphos- phanyl-propan-2-yl)oxy]-calix[4]arene via stereospecific methylation on Evans' oxazolidinone moiety was reported. According to the 13 C NMR analysis of this phosphine, the calix[4]arene skeleton adopted a 1,3-alternate conformation. The latter conformation of the macrocycle and the ( S )-chirality of the carbon atom bearing the methyl substituent were confirmed by a single-crystal X-ray diffraction study. After coordination of the phosphinated ligand to the dimeric [RuCl2 ( p -cymene)]2 organometallic precursor, the resulting arene-ruthenium complex was tested in the asymmetric reduction of acetophenone and alcohol was obtained with modest enantiomeric excess...
March 5, 2024: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/38438563/in-vitro-activity-of-tedizolid-against-43-species-of-nocardia-species
#5
JOURNAL ARTICLE
Masahiro Toyokawa, Noboru Ohana, Daiki Tanno, Minako Imai, Yukiko Takano, Kazutaka Ohashi, Tomonari Yamashita, Kyoichi Saito, Hiroki Takahashi, Hiroki Shimura
The purpose of the present study was to evaluate the in vitro activity of tedizolid against several clinically significant species of Nocardia by comparing with that of linezolid. A total of 286 isolates of Nocardia species, including 236 clinical isolates recovered from patients in Japan and 50 strains (43 species) purchased from NITE Biological Resource Center, were studied. Antimicrobial susceptibility testing was performed using the broth microdilution method. For the 286 Nocardia isolates, the minimal inhibitory concentration (MIC)50 and MIC90 values of tedizolid were 0...
March 4, 2024: Scientific Reports
https://read.qxmd.com/read/38436463/pharmacokinetic-and-pharmacodynamic-modeling-analysis-of-delpazolid-lcb01-0371-in-adult-patients-with-pulmonary-tuberculosis
#6
JOURNAL ARTICLE
Sang Min Lee, Seung Chan Choi, Kyung Ran Mun, Ji Young Seo, Young Lag Cho, Tae Sun Shim, Hyeong-Seok Lim
Delpazolid (LCB01-0371) is a novel oxazolidinone derivative with a good safety profile for treating gram-positive pathogenic infections such as Mycobacterium abscessus, a highly pathogenic drug-resistant Mycobacterium. In this study, we evaluated the pharmacokinetics (PK) and pharmacodynamics (PD) of delpazolid after 14 days of multiple oral administration, using data from adult patients with pulmonary tuberculosis. 800 mg once a day, 400 mg twice a day, 800 mg twice a day, and 1200 mg once a day delpazolid for 14 days were tested in 63 patients with pulmonary tuberculosis...
March 4, 2024: Journal of Clinical Pharmacology
https://read.qxmd.com/read/38434706/adverse-drug-events-associated-with-linezolid-administration-a-real-world-pharmacovigilance-study-from-2004-to-2023-using-the-faers-database
#7
JOURNAL ARTICLE
Fan Zou, Zhiwei Cui, Siyu Lou, Yingyong Ou, Chengyu Zhu, Chengjie Shu, Junyou Chen, Ruizhen Zhao, Zhu Wu, Li Wang, Zhenyong Chen, Huayu Chen, Yuanbo Lan
Introduction: Linezolid is an oxazolidinone antibiotic that is active against drug-resistant Gram-positive bacteria and multidrug-resistant Mycobacterium tuberculosis . Real-world studies on the safety of linezolid in large populations are lacking. This study aimed to determine the adverse events associated with linezolid in real-world settings by analyzing data from the US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS). Methods: We retrospectively extracted reports on adverse drug events (ADEs) from the FAERS database from the first quarter of 2004 to that of 2023...
2024: Frontiers in Pharmacology
https://read.qxmd.com/read/38415968/photo-and-cobalt-catalyzed-synthesis-of-heterocycles-via-cycloisomerization-of-unactivated-olefins
#8
JOURNAL ARTICLE
Henry Lindner, Willi M Amberg, Tristano Martini, David M Fischer, Eléonore Moore, Erick Moran Carreira
We report a general, intramolecular cycloisomerization of unactivated olefins with pendant nucleophiles. The reaction proceeds under mild conditions and tolerates ethers, esters, protected amines, acetals, pyrazoles, carbamates, and arenes. It is amenable to N-, O-, as well as C-nucleophiles, yielding a number of different heterocycles including, but not limited to, pyrrolidines, piperidines, oxazolidinones, and lactones. Use of both a benzothiazinoquinoxaline as organophotocatalyst and a Co-salen catalyst obviates the need for stoichiometric oxidant or reductant...
February 28, 2024: Angewandte Chemie
https://read.qxmd.com/read/38415667/population-pharmacokinetic-rationale-for-intravenous-contezolid-acefosamil-followed-by-oral-contezolid-dosage-regimens
#9
JOURNAL ARTICLE
Jürgen B Bulitta, Edward Fang, Martin E Stryjewski, Wen Wang, George J Atiee, Jeffrey G Stark, Barry Hafkin
Contezolid is a novel oxazolidinone antibiotic with a promising safety profile. Oral contezolid and its intravenous (IV) prodrug contezolid acefosamil (CZA) are in development for treatment of diabetic foot and acute bacterial skin and skin structure infections (ABSSSI). The prodrug CZA is converted to active contezolid via intermediate MRX-1352. This study aimed to provide the pharmacokinetic rationale for safe, effective, and flexible dosage regimens with initial IV CZA followed by oral contezolid. We simultaneously modeled plasma concentrations from 110 healthy volunteers and 74 phase 2 patients with ABSSSI via population pharmacokinetics (using the importance sampling estimation algorithm), and optimized dosage regimens by Monte Carlo simulations...
February 28, 2024: Antimicrobial Agents and Chemotherapy
https://read.qxmd.com/read/38407341/diastereoselective-access-to-c-c-glycosyl-amino-acids-via-iron-catalyzed-auxiliary-enabled-mhat-coupling
#10
JOURNAL ARTICLE
Mylène Lang, Damien Tardieu, Benoit Pousse, Philippe Compain, Nicolas Kern
Access to C , C -glycosyl amino acids as a novel class of glycomimetics is reported by means of radical generation, intermolecular addition and stereoselective reduction via a metal-induced hydrogen atom transfer (MHAT) sequence. The 'matched' coupling of exo -D-glycals with an enantiopure dehydroalanine bearing a ( R )-configured benzyl oxazolidinone enables a singular case of two-fold diastereocontrol under iron catalysis. In the common exo -D-glucal series, the nature of the C-2 substituent was found to play a key role from both reactivity and stereocontrol aspects...
February 26, 2024: Chemical Communications: Chem Comm
https://read.qxmd.com/read/38389893/design-synthesis-and-antiproliferative-evaluation-of-novel-dehydroabietic-acid-1-2-3-triazole-oxazolidinone-hybrids
#11
JOURNAL ARTICLE
Yaju Wu, Lin Huang, Xianli Ma, Xiaoqun Zhou, Qian Li, Fangyao Li
A series of novel dehydroabietic acid derivatives containing both 1,2,3-triazole and oxazolidinone 4a-4t have been synthesized and their antiproliferative activity in vitro against HeLa, HepG2, MGC-803 and T-24 cell lines evaluated. Most of them displayed cell proliferation inhibition on four tested human malignant tumour cell lines to some degree. Among them, compound 4p exhibited promising cytotoxicity with IC50 values ranging from 3.18 to 25.31 μM and weak cytotoxicity toward normal cells. The mechanism of action of 4p was then studied using flow cytometry, Hoechst 33258 staining, ROS generation assay, and JC-1 mitochondrial membrane potential staining, which illustrated that compound 4p induced apoptosis, arrested mitotic process at the G1 phase of the cell cycle, reduced the mitochondrial membrane potential, and increased intracellular ROS levels...
February 21, 2024: RSC medicinal chemistry
https://read.qxmd.com/read/38384659/compassionate-use-of-contezolid-in-a-toddler-with-severe-community-acquired-pneumonia-induced-by-staphylococcus-aureus-a-case-report-and-follow-up
#12
Hui-Ying Liu, Xiao-Fei Bi, Ya-Jun Wang, Feng-Jie Xie, Hong Zhang, Yu-Cheng Zhu, Yan Zhang, Zhi-Hui Wang, Di Wu, Huan Meng, Yi-Lu Lin, Lin-Qiong Liu, Shu-Xiao Qiu, Yan Gao, Kai Kang, Yang Gao
BACKGROUND: Initial choices of antimicrobial therapy for most cases of community-acquired pneumonia (CAP) in children under 5 years of age are typically based on local epidemiology, risk factors assessment, and subsequent clinical parameters and positive cultures, which can lead to the underdiagnosis and underestimation of lung infections caused by uncommon pathogens. Contezolid, an orally administered oxazolidinone antibiotic, gained approval from the National Medical Products Administration (NMPA) of China in June 2021 for managing complicated skin and soft tissue infections (cSSTI) caused by staphylococcus aureus (SA), streptococcus pyogenes, or streptococcus agalactis...
2024: Frontiers in Pediatrics
https://read.qxmd.com/read/38376228/bactericidal-and-sterilizing-activity-of-novel-regimens-combining-bedaquiline-or-tbaj-587-with-gsk2556286-and-tba-7371-in-a-mouse-model-of-tuberculosis
#13
JOURNAL ARTICLE
Si-Yang Li, Sandeep Tyagi, Heena Soni, Fabrice Betoudji, Paul J Converse, Khisimuzi Mdluli, Anna M Upton, Nader Fotouhi, David Barros-Aguirre, Lluís Ballell, Elena Jimenez-Navarro, Eric L Nuermberger
The combination of bedaquiline, pretomanid, and linezolid (BPaL) has become a preferred regimen for treating multidrug- and extensively drug-resistant tuberculosis (TB). However, treatment-limiting toxicities of linezolid and reports of emerging bedaquiline and pretomanid resistance necessitate efforts to develop new short-course oral regimens. We recently found that the addition of GSK2556286 increases the bactericidal and sterilizing activity of BPa-containing regimens in a well-established BALB/c mouse model of tuberculosis...
February 20, 2024: Antimicrobial Agents and Chemotherapy
https://read.qxmd.com/read/38364367/comparison-of-plasma-concentration-of-linezolid-s-detection-by-fica-and-lc-ms-ms
#14
JOURNAL ARTICLE
Jing Chen, Chenxia Zhu, Yangjin He, Hengbin Cao
Linezolid was the first totally synthetic oxazolidinone antibiotic that was approved for clinical use against Mycobacterium tuberculosis. Our study investigated the correlation and consistency of fluorescence immunochromatography assay (FICA) and high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) in measuring linezolid levels in the plasma. Plasma samples were collected from 80 to 100 tuberculosis patients. The samples were analyzed by FICA and LC-MS/MS, and linezolid levels measured by the two methods were compared by outlier test, correlation coefficient, Bland-Altman scatter plot, Deming regression analysis and bias evaluation...
February 13, 2024: Journal of Chromatographic Science
https://read.qxmd.com/read/38354645/rapid-determination-of-furazolidone-residues-in-animal-foods-by-time-resolved-fluorescence-immunochromatography
#15
JOURNAL ARTICLE
Yongsong Zhou, Jingneng Wang, Buling Wu, Bofeng Zhu
Although furazolidone (FZD) was completely banned from livestock production in many countries many years ago due to its mutagenicity and carcinogenicity, the abuse of FZD is still common today. Accurate and rapid detection of FZD residues in animal-derived food products is highly important for human health. Here, a time-resolved fluorescence immunochromatography (TRFI) test strip for rapid and quantitative detection of 3-amino-2-oxazolidinone (AOZ) residues in animal foods was developed and validated. Its limit of detection and limit of quantification were 0...
February 10, 2024: Food Chemistry
https://read.qxmd.com/read/38337267/gold-nanoclusters-synthesized-within-single-chain-nanoparticles-as-catalytic-nanoreactors-in-water
#16
JOURNAL ARTICLE
Jokin Pinacho-Olaciregui, Ester Verde-Sesto, Daniel Taton, José A Pomposo
Metalloenzymes are able to catalyze complex biochemical reactions in cellular (aqueous) media with high efficiency. In recent years, a variety of metal-containing single-chain nanoparticles (SCNPs) have been synthesized as simplified metalloenzyme-mimetic nano-objects. However, most of the metal-containing SCNPs reported so far contained complexed metal ions but not metal nanoclusters (NCs) with diameter <5 nm, which could be used as powerful, emerging catalysts. Herein, we report the synthesis of gold nanoclusters (Au-NCs) within SCNPs and the further use of Au-NCs/SCNPs as catalytic nanoreactors in water...
January 30, 2024: Polymers
https://read.qxmd.com/read/38336230/which-trial-do-we-need-empiric-glycopeptides-plus-clindamycin-versus-oxazolidinones-for-suspected-toxic-shock-and-necrotizing-soft-tissue-infections-toxic-ego
#17
JOURNAL ARTICLE
Joshua Osowicki, Fergus Hamilton, Todd C Lee, Michael Marks, Erin K McCreary, Emily G McDonald, Jonathan H Ryder, Steven Yc Tong
No abstract text is available yet for this article.
February 7, 2024: Clinical Microbiology and Infection
https://read.qxmd.com/read/38336229/transferable-linezolid-resistance-genes-optra-and-poxta-in-enterococci-derived-from-livestock-compost-at-japanese-farms
#18
JOURNAL ARTICLE
Akira Fukuda, Chie Nakajima, Yasuhiko Suzuki, Masaru Usui
OBJECTIVES: Linezolid is a last-resort antimicrobial in human clinical settings to treat multidrug-resistant gram-positive bacterial infections. Mobile linezolid resistance genes (optrA, poxtA, and cfr) have been detected in various sources worldwide. However, the presence of linezolid-not-susceptible bacteria and mobile linezolid resistance genes in Japan remains uncertain. Therefore, we clarified the existence of linezolid-not-susceptible bacteria and mobile linezolid resistance genes in farm environments in Japan...
February 7, 2024: Journal of Global Antimicrobial Resistance
https://read.qxmd.com/read/38285535/synthesis-of-s-iv-stereogenic-chiral-thio-oxazolidinones-via-palladium-catalyzed-asymmetric-3-2-annulations
#19
JOURNAL ARTICLE
Bao-Cheng Wang, Fang Hu, Jiahui Bai, Fen-Ya Xiong, Peng Chen, Jianye Li, Ying Tan, Yin-Long Guo, Wen-Jing Xiao, Liang-Qiu Lu
Organic molecules bearing chiral sulfur stereocenters exert a great impact on asymmetric catalysis and synthesis, chiral drugs, and chiral materials. Compared with acyclic ones, the catalytic asymmetric synthesis of thio-heterocycles has largely lagged behind due to the lack of efficient synthetic strategies. Here we establish the first modular platform to access chiral thio-oxazolidinones via Pd-catalyzed asymmetric [3+2] annulations of vinylethylene carbonates with sulfinylanilines. This protocol is featured by readily available starting materials, and high enantio- and diastereoselectivity...
January 29, 2024: Angewandte Chemie
https://read.qxmd.com/read/38259199/pyrene-based-nanoporous-covalent-organic-framework-for-carboxylation-of-c-h-bonds-with-co-2-and-value-added-2-oxazolidinones-synthesis-under-ambient-conditions
#20
JOURNAL ARTICLE
Gulshan Singh, Nidhi Duhan, T J Dhilip Kumar, C M Nagaraja
The selective carbon capture and utilization (CCU) as a one-carbon (C1) feedstock offers dual advantages for mitigating the rising atmospheric CO2 content and producing fine chemicals/fuels. In this context, herein, we report the application of a porous bipyridine-functionalized, pyrene-based covalent organic framework (Pybpy-COF) for the stable anchoring of catalytic Ag(0) nanoparticles (NPs) and its catalytic investigation for fixation of CO2 to commodity chemicals at ambient conditions. Notably, Ag@Pybpy-COF showed excellent catalytic activity for the carboxylation of various terminal alkynes to corresponding alkynyl carboxylic acids/phenylpropiolic acids via C-H bond activation under atmospheric pressure conditions...
January 23, 2024: ACS Applied Materials & Interfaces
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