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Acetamides (7):
Recent article
Acetamides
Abstract
The effects of (Rac)-metolachlor and (S)-metolachlor on the avoidance behavior, bodyweight change and in vivo enzyme activity of earthworms (Eisenia foetida) were determined and compared in this study. The effects of (Rac)-metolachlor on the enzyme activities of E. foetida and bodyweight were more s...
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PMID: 20723980
PDF is available here.
PDF is available here.
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Biochemical Journal (432)1 2010
Abstract
We investigated the role of the ERK (extracellular-signal-regulated kinase) and p38 MAPK (mitogen-activated protein kinase) signalling pathways in MEL (mouse erythroleukaemia) cell differentiation. We found that treatment of HMBA (hexamethylene bisacetamide)-induced MEL cells with the ERK pathway in...
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PMID: 20738258
PDF is available here.
PDF is available here.
MMW Fortschritte der Medizin (152)40 2010
Abstract
Abstract
A current study shows that sodium dichloroacetate (DCA) can induce cancer cell apoptosis and inhibit tumor growth, but its cytotoxic activity is low (IC(50) > 1000 microM for A549). In this paper, a variety of DCA derivatives were synthesized, and their cytotoxic activities were evaluated. The resul...
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PMID: 20663593
PDF is available here.
PDF is available here.
Abstract
Two studies in hydrocephalic children and adolescents were performed to assess the penetration of linezolid into cerebrospinal fluid and its relation to meningeal inflammation.
Each patient was administered intravenous linezolid 10 mg/kg every 12 hours for 3 days (study 1) or every 8 hours for 2 day...
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PMID: 20442688
PDF is available here.
PDF is available here.
Abstract
We postulated that CRMP-2 levels affects the actions of LCM on VGSCs. CRMP-2 labeling by LCM analogs was competitively displaced by excess LCM in rat brain lysates. Manipulation of CRMP-2 levels in the neuronal model system CAD cells affected slow inactivation of VGSCs without any effects on other v...
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PMID: 20538611
PDF is available here.
PDF is available here.
Chemmedchem (5)8 2010
Abstract
Abstract
Rats with oxygen-induced retinopathy (OIR) model the pediatric retinal disease retinopathy of prematurity (ROP). Recent findings in OIR rats imply a causal role for the rods in the ROP disease process, although only experimental manipulation of rod function can establish this role conclusively. Acco...
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PMID: 20430026
PDF is available here.
PDF is available here.
Abstract
We have determined important molecular determinants of the ligand-binding pocket of OX(1) and OX(2). The conserved residues Asp(45.51), Trp(45.54), Tyr(5.38), Phe(5.42), Tyr(5.47), Tyr(6.48), and His(7.39) were found to be contributing to both orexin-A-binding sites at OX(1) and OX(2). Among these c...
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PMID: 20404073
PDF is available here.
PDF is available here.
Abstract
Abstract
Abstract
These results indicate that agomelatine reversed the neuroplastic changes and helpless behaviour associated with HPA axis alterations in GR-i mice, suggesting neurobiological and behavioural effects mostly similar to those typically seen with classical antidepressants such as fluoxetine, but through...
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PMID: 19775499
PDF is available here.
PDF is available here.
Abstract
Concentrations of atrazine and metolachlor and stereoisomer fractions (SF = herbicidally active/total stereoisomers) of metolachlor were determined in 101 surface water samples collected from the five Laurentian Great Lakes in 2005-2006. Geometric mean (GM) concentrations of atrazine ranged from 5.5...
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PMID: 20504016
PDF is available here.
PDF is available here.
Abstract
The first clinical outbreak, to our knowledge, with LRSA mediated by the cfr gene developed at our center, was associated with nosocomial transmission and extensive usage of linezolid. Reduction of linezolid use and infection-control measures were associated with the termination of the outbreak....
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PMID: 20530779
PDF is available here.
PDF is available here.
Abstract
Abstract
OBT is sensitive for potentially evaluating liver function in rat models of acute hepatitis and thioacetamide-induced liver cirrhosis but not in cholestatic liver injury. The MBID test may be better for evaluation of cholestatic liver disease in this model....
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PMID: 19731033
PDF is available here.
PDF is available here.
Abstract
We report such a case in a 25-year-old man who presented with an intermittent fever. He had a history of prolonged antibiotic use for acne and skin abscesses. The liver abscess was successfully treated with percutaneous drainage and a prolonged course of linezolid. To our knowledge, this is the firs...
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PMID: 20519761
PDF is available here.
PDF is available here.
Abstract
To demonstrate the clinical effectiveness of an antidepressant drug requires evidence beyond short- and long-term efficacy, including a favourable adverse-effect profile and sustained treatment adherence. Under these conditions, patients should experience enhanced social and functional outcomes. The...
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PMID: 20192279
PDF is available here.
PDF is available here.
Abstract
We screened the precursors of dichloroacetamide (DCAcAm), the most commonly identified HAcAm in chlorinated or chloraminated drinking water. DCAcAm formation potential (FP) of raw water samples collected in different months from a reservoir in China was determined during chlorination, and the highes...
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PMID: 20397690
PDF is available here.
PDF is available here.
Abstract
High-throughput screening identified compound 1 as a potent P2X(7) receptor antagonist suitable for lead optimisation. Structure-activity relationships (SAR) of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified as a potent P2X(7) antagonist with enhanced potenc...
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PMID: 20399651
PDF is available here.
PDF is available here.
Analytica Chimica Acta (667)1-2 2010
Abstract
Simple or even rapid bioanalytical methods are rare, since they generally involve complicated, time-consuming sample preparation from the biological matrices like LLE or SPE. SPME provides a promising approach to overcome these limitations. The full potential of this innovative technique for medical...
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PMID: 20441869
PDF is available here.
PDF is available here.
Abstract
Proteomics analysis showed that 43 protein spots were significantly changed due to HMBA treatment. Fifteen proteins were identified in the HMBA-induced differentiation of gastric tumor cells. Eight proteins spots were down-regulated while seven were up-regulated. Among these proteins, prohibitin, nu...
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PMID: 20440860
PDF is available here.
PDF is available here.
Abstract
We show that this radiotracer has a high in vitro specificity for PBR/TSPO versus central benzodiazepine receptors, as reflected by the drastic reduction of its binding to target tissue by addition of PK11195 or PBR111, while addition of flumazenil does not affect binding. Only intact [(18)F]PBR111...
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PMID: 20069292
PDF is available here.
PDF is available here.
Abstract
To evaluate the efficacy, safety, and tolerability of fixed-dose agomelatine 25 and 50 mg/d in the treatment of outpatients with moderate-to-severe major depressive disorder (MDD) compared to placebo.
In this 8-week, multicenter, double-blind, parallel-group trial, patients with DSM-IV-defined MDD w...
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PMID: 20361916
PDF is available here.
PDF is available here.
Abstract
In recent years, coagulase-negative staphylococci (CoNS) have been increasingly recognised as causative agents of various infections, especially in immunocompromised patients and related to implanted foreign body materials. CoNS, and especially Staphylococcus epidermidis, transform into a stationary...
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PMID: 20221891
PDF is available here.
PDF is available here.
Abstract
The in vitro activity of TR-700 (torezolid) was evaluated against a collection of 660 staphylococcal blood isolates. TR-700 showed excellent activity against all the staphylococci tested. The MIC(50) and MIC(90) values of TR-700, linezolid, daptomycin, and vancomycin against methicillin-resistant St...
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PMID: 20176900
PDF is available here.
PDF is available here.
Abstract
We describe a fast standardized 9-day acute assay intended to measure the efficacy of drugs against M. tuberculosis growing in the lungs of immunocompetent mice. This assay is highly reproducible, allows good throughput, and was validated for drug lead optimization using isoniazid, rifampin, ethambu...
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PMID: 20160054
PDF is available here.
PDF is available here.
Abstract
We developed two cellular reporter assays and applied them to a library of 80,000 compounds. The primary screen was based on the dependence of the transcription of T3SS operons on the T3SS-mediated secretion of a negative regulator and consisted of a transcriptional fusion of the Photorhabdus lumine...
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PMID: 20176902
PDF is available here.
PDF is available here.
Abstract
Synergy time-kill studies of 47 methicillin-resistant Staphylococcus aureus strains with differing resistance phenotypes showed that combinations of subinhibitory concentrations of ACHN-490 and daptomycin yielded synergy against 43/47 strains at 24 h, while the combination was indifferent against th...
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PMID: 20145088
PDF is available here.
PDF is available here.
Abstract
Relative gas-phase carbon acidities have been computed for a series of acetamides, diketopiperazines, and linear dipeptides. The results show that N-electron-withdrawing substituents, protonation, and hydrogen bonding at amide nitrogen in these systems increase the acidity of both a C-H proton adjac...
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PMID: 20337444
PDF is available here.
PDF is available here.
Ugeskrift for laeger (172)16 2010
Abstract
In Denmark enterococci causes 15 to 20% of all endocarditis (IE) cases. The development of multi-resistant bacterial strains has increased the need for new antibiotics. Linezolid is an alternative to conventional treatment of infections with gram positive cocci. In this case report linezolid was use...
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PMID: 20423667
PDF is available here.
PDF is available here.
Abstract
We report the clinical course of a patient with bitemporal epilepsy who ingested 12 g of lacosamide, 56 g of gabapentin, 2g of topiramate, and 2.8 g of zonisamide during a suicide attempt. The patient was found comatose and experienced repeated generalized tonic-clonic seizures, aspiration with subs...
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PMID: 20171144
PDF is available here.
PDF is available here.
Psychopharmacology (209)2 2010
Abstract
These data confirm a previous report (Hollander et al., Proc Natl Acad Sci U S A 105:19480-19485, 2008) that the hypocretin receptor hcrtR1 is activated in nicotine reinforcement and in addition show that both the arcuate nucleus and lateral hypothalamus are sites at which hcrt receptor mechanisms m...
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PMID: 20177882
PDF is available here.
PDF is available here.
Abstract
Biolabile 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides 34-42 have been synthesized and evaluated for their in vitro antibacterial and antifungal activities. The minimum inhibitory concentration tested for the same compounds against the same set of bacterial and fungal strains shows that the c...
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PMID: 20106563
PDF is available here.
PDF is available here.
Journal of Environmental Science and Health, Part B: Pesticides, Food Contaminants and Agricultural Wastes (45)3 2010
Abstract
We investigated its enantioselective interactions, and that of its (S)-isomer, with Penicillium expansum alkaline lipase and phosphatase. UV differential spectroscopy and fluorescence spectrophotometry studies were conducted in phosphate buffered solution at pH 7. Chiral differences in the UV absorp...
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PMID: 20390958
PDF is available here.
PDF is available here.
Abstract
The purpose of this study was to assess lipopolysaccharide (LPS)-stimulated cytokine production in the presence of linezolid (LZD) in comparison with the drug effect on the plasma endotoxin level. Peripheral venous whole-blood samples collected from five healthy subjects were stimulated with 10 micr...
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PMID: 20094752
PDF is available here.
PDF is available here.
Abstract
26 patients with unilateral postoperative endophthalmitis with a systemic combination regimen of meropenem (2 g TID, mean duration of treatment 5.5 days) and linezolid (600 mg BID, mean duration of treatment 8.9 days) (group 1, mean follow-up time 140 days) were included in this study and compared t...
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PMID: 20408069
PDF is available here.
PDF is available here.
Abstract
MRSA is one of the most common pathogens of ventilator associated pneumonia, whereas its estimated incidence for hospital acquired pneumonia, healthcare associated pneumonia and community acquired pneumonia has risen in the past decades. Although vancomycin at standard doses remains as the mainstay...
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PMID: 20075728
PDF is available here.
PDF is available here.
Abstract
A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with thioether acetamide functional groups were prepared with the goal of improving upon the cellular activity of amidoethylthioethers. This Letter describes altered amide connectivity, in conjunction with changes to other binding e...
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PMID: 20188543
PDF is available here.
PDF is available here.
Abstract
Soil incubation and germination tests were conducted to assess zerovalent iron (ZVI), organic compost, moisture and their combinations on metolachlor degradation in soil. The ZVI alone degraded 91% of metolachlor in soil within 40 days following bi-phasic kinetics. Organic amendment alone facilitate...
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PMID: 20352186
PDF is available here.
PDF is available here.
Abstract
We exposed three common species of tadpoles to conservative levels of atrazine, S-metolachlor, and glyphosate end-use herbicide formulations throughout the larval period to test for survival differences or life-history trait alterations. Exposure to the glyphosate product Roundup WeatherMax at 572 p...
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PMID: 19768486
PDF is available here.
PDF is available here.
Abstract
We present the relative risks of a variety of exposure scenarios and recovery potentials from damage, using herbicides with different modes of action. Toxicity was assessed on the basis of both EC50 and relative growth rate (RGR) compared with untreated controls in exposure and recovery. The EC50 of...
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PMID: 20094883
PDF is available here.
PDF is available here.
MMW Fortschritte der Medizin (152)10 2010
Abstract
Abstract
A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta(3)-AR agonists for the treatment of overactive bladder.
Copyright 2010 Elsevier...
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PMID: 20181479
PDF is available here.
PDF is available here.
Abstract
We experimentally searched for other organic molecules of prebiotic interest, namely, oxidized acid labile compounds. In a setup that simulates conditions relevant to the ISM and Solar System icy bodies such as comets, a condensed CH(3)OH:NH(3) = 1:1 ice mixture was UV irradiated at approximately 80...
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PMID: 20402585
PDF is available here.
PDF is available here.
Abstract
Our results suggest that linezolid pharmacokinetics in critically ill patients with ARF undergoing ED is not comparable to that in healthy subjects and patients without ARF. The best method of managing linezolid dosage in such a complex group of patients, whose physiology can vary daily, would be to...
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PMID: 20013257
PDF is available here.
PDF is available here.
Abstract
The method offers a fast and simple approach to determine linezolid in pulmonary tissue which could be of use in pharmacokinetic studies....
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PMID: 20113250
PDF is available here.
PDF is available here.
Abstract
This study reports the synthesis and antioxidant activity of some new acetamide derivatives. The compounds' structures were elucidated by NMR analysis and their melting points were measured. The in vitro antioxidant activity of these compounds was tested by evaluating the amount of scavenged ABTS ra...
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PMID: 20336030
PDF is available here.
PDF is available here.
Abstract
A novel series of dual orexin receptor antagonists was prepared by heteroaromatic five-membered ring system replacement of the dimethoxyphenyl moiety contained in the tetrahydroisoquinoline core skeleton of almorexant. Thus, replacement of the dimethoxyphenyl by a substituted pyrazole and additional...
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PMID: 20144866
PDF is available here.
PDF is available here.
Abstract
In the absence of clinical data correlating ELF concentrations and clinical outcome, the clinical significance of differences in pulmonary penetration of vancomycin and linezolid is unknown. Higher vancomycin serum concentrations may be necessary to achieve appropriate lung concentrations to optimiz...
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PMID: 20055750
PDF is available here.
PDF is available here.
Abstract
A total of 565 methicillin-resistant Staphylococcus aureus (MRSA) isolates were collected mostly from Europe and the Americas (2004 to 2007) during a phase IV clinical trial comparing linezolid with vancomycin for the treatment of complicated skin and skin structure infections proven to be due to MR...
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PMID: 19940054
PDF is available here.
PDF is available here.
Abstract
Abstract
We retrospectively evaluated 410 patients with coinfection or cocolonization due to vancomycin-resistant (VR) enterococcus (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). The prevalence rate was 19.8%. Risk factors included isolation of VR Enterococcus faecalis and use of linezolid or...
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PMID: 20007403
PDF is available here.
PDF is available here.
Abstract
The favorable effect of agomelatine on the relative amplitude of the circadian rest-activity/sleep-wake cycle in depressed patients at week 1 reflects early improvement in sleep and daytime functioning. Higher efficacy results were observed with agomelatine as compared to sertraline on both depressi...
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PMID: 20193645
PDF is available here.
PDF is available here.
Abstract
A total of 26 pharmacokinetic profiles were obtained. The median AUC0-12h was 51.8 (interquartile range, 41.8-65.9) mg*h/L at 300 mg and 123.8 (interquartile range, 100.9-152.5) mg*h/L at 600 mg, both twice daily. The most relevant model clinically for prediction of linezolid AUC0-12h used a linezol...
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PMID: 20042919
PDF is available here.
PDF is available here.
Pediatric Emergency Care (26)2 2010
Abstract
We present a case of a fully immunized 20-month-old boy with Streptococcus pneumoniae posttraumatic septic arthritis without evidence of an open fracture....
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PMID: 20145504
PDF is available here.
PDF is available here.
Journal of Chemotherapy (22)1 2010
Abstract
The aim of the study was to evaluate the penetration of linezolid into cerebrospinal fluid (CSF) and brain tissue after a single i.v. dose of 600 mg. The penetration of linezolid into cerebrospinal fluid and brain tissue was studied in 18 patients undergoing a neurosurgical procedure. Linezolid 600...
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PMID: 20227987
PDF is available here.
PDF is available here.
Abstract
The ability of melatonin to shift biological rhythms is well known. As a result, melatonin has been used in the treatment of various circadian rhythm sleep disorders, such as advanced and delayed sleep phase disorders, jet lag and shiftwork disorder. The current evidence for melatonin being efficaci...
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PMID: 20136385
PDF is available here.
PDF is available here.
Clinical calcium (20)2 2010
Abstract
Androgen, one of the sex steroid hormones shows various biological activities on the corresponding various tissues. Many efforts to produce novel drug materials maintaining a desired biological activity with an adequate tissue selectivity, which is so-called selective androgen receptor modulators (S...
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PMID: 20118515
PDF is available here.
PDF is available here.