253 research outputs found
(E)-3-Heteroarylidenechroman-4-ones as potent and selective monoamine oxidase-B inhibitors
A series of (E)-3-heteroarylidenechroman-4-ones (1a-r) was designed, synthesized and investigated
in vitro for their ability to inhibit the enzymatic activity of both human monoamine oxidase (hMAO)
isoforms, hMAO-A and hMAO-B. All the compounds were found to be selective hMAO-B inhibitors
showing IC50 values in the nanomolar or micromolar range. (E)-5,7-Dichloro-3-{[(2-(dimethylamino)
pyrimidin-5-yl]methylene}chroman-4-one (1c) was the most interesting compound identified in this
study, endowed with higher hMAO-B potency (IC50 ¼ 10.58 nM) and selectivity (SI > 9452) with respect
to the reference selective inhibitor selegiline (IC50 ¼ 19.60 nM, IC50 > 3431). Molecular modelling studies
were performed for rationalizing at molecular level the target selective inhibition of our compounds,
revealing a remarkable contribution of hydrogen bond network and water solvent
HYDROGEN-BONDED SUPRAMOLECULAR ARRAY IN THE CRYSTAL STRUCTURE OF ETHYL 7-HYDROXY-2-OXO-2H-CHROMENE-3-CARBOXYLATE MONOHYDRATE
Indexación: Web of Science; ScieloThe crystal structure of ethyl 7-hydroxy-2-oxo-2H-chromene-3-carboxylate monohydrate (1), C12H10O5.H2O, was established by X-ray crystallographic analysis. The molecule of the title compound is essentially planar except for the carboxylate substituent group. The crystal packing supramolecular array arises from hydrogen bonds and intermolecular C-H - O=C contacts of the organic molecules and solvent water molecules, with graph-set descriptor R24 (8), R21 (6), R44 ( 20) and C (5) motifs. The water molecules are involved as donors and acceptors. The hydrogen bond and intermolecular interaction network is reinforced by stacking of the sheet through p-p interactions.http://ref.scielo.org/qhfkn
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Narrative Review of Incremental Hemodialysis.
The prescription of hemodialysis (HD) in patients with incident end-stage kidney disease (ESKD) is fundamentally empirical. The abrupt transition from nondialysis chronic kidney disease (CKD) to thrice-weekly in-center HD of much the same dialysis intensity as in those with prevalent ESKD underappreciates the progressive nature of kidney disease whereby the decline in renal function has been gradual and ongoing-including at the time of HD initiation. Adjuvant pharmacologic treatment (i.e., diuretics, acid buffers, potassium binders), coupled with residual kidney function (RKF), can complement an initial HD regimen of lower intensity. Barriers to less intensive HD in incident ESKD include risk of inadequate clearance of uremic toxins due to variable and unexpected loss of RKF, lack of patient adherence to assessments of RKF or adjustment of HD intensity, increased burden for all stakeholders in the dialysis units, and negative financial repercussions. A stepped dialysis regimen with scheduled transition from time-delineated twice-weekly HD to thrice-weekly HD could represent an effective and safe strategy to standardize incremental HD in patients with CKD transitioning to early-stage ESKD. Patients' adherence and survival as well as other clinical outcomes should be rigorously evaluated in clinical trials before large-scale implementation of different incremental schedules of HD. This review discusses potential benefits of and barriers to alternative dialysis regimens in patients with incident ESKD, with emphasis on twice-weekly HD with pharmacologic therapy, and summarizes in-progress clinical trials of incremental HD schedules
Evaluation of bacteriological and chemical quality of dialysis water and fluid in Isfahan, central Iran
Background: Chemical and microbial quality of water used in hemodialysis play key roles in a number of dialysisrelated complications. In order to avoid the complications and to guarantee safety and health of patients therefore, vigorous control of water quality is essential. The objective of present study was to investigate the chemical and bacteriological characteristics of water used in dialysis centers of five hospitals in Isfahan, central Iran. Methods: A total of 30 water samples from the input of dialysis purification system and dialysis water were analyzed for chemical parameters. Heterotrophic plate count and endotoxin concentration of drinking water, dialysis water and dialysis fluid of 40 machines were also monitored over a 5-month period in 2011-2012. Results: Concentration of the determined chemicals (copper, zinc, sulfate, fluoride, chloramines and free chlorine) did not exceed the recommended concentration by the Association for the Advancement of Medical Instrumentation (AAMI) exclude lead, nitrate, aluminum and calcium. Furthermore, the magnesium; cadmium and chromium concentration exceeded the maximum level in some centers. No contamination with heterotrophic bacteria was observed in all samples, while the AMMI standard for endotoxin level in dialysis fluid (<2 EU/ml) was achieved in 95 of samples. Conclusion: Dialysis water and fluid failed to meet the all chemical and bacteriological requirements for hemodialysis. To minimize the risk of contaminants for hemodialysis patients therefore, a water quality management program including monitoring, maintenance and development of water treatment system in hemodialysis centers is extremely important. In addition, an appropriate disinfection program is needed to guarantee better control of bacterial growth and biofilm formation. © 2016, Iranian Journal of Public Health. All rights reserved
Thrice weekly nocturnal in-centre haemodiafiltration: a 2-year experience
Background: Adequate control of plasma phosphate without phosphate binders is difficult to achieve on a thrice-weekly haemodialysis schedule. The use of quotidian nocturnal dialysis is effective but not practical in the in-centre setting. This quality improvement project was set up as an exercise allowing the evaluation of small-solute clearance by combining convection with extended-hour dialysis in a thrice-weekly hospital setting. Methods: A single-centred, prospective analysis of patients' electronic records was performed from August 2012 to July 2014. The duration of haemodiafiltration was increased from a median of 4.5 to 8 h. Dialysis adequacy, biochemical parameters and medications were reviewed on a monthly basis. A reduction in plasma phosphate was anticipated, so all phosphate binders were stopped. Results: Since inception, 14 patients have participated with over 2,000 sessions of dialysis. The pre-dialysis phosphate level fell from a mean of 1.52 ± 0.4 to 1.06 ± 0.1 mmol/l (p < 0.05). The average binder intake of 3.26 ± 2.6 tablets was eliminated. A normal plasma phosphate range has been maintained with increased dietary phosphate intake and no requirement for intradialytic phosphate supplementation. Conclusion: Phosphate control can be achieved without the need for binders or supplementation on a thrice-weekly in-centre haemodiafiltration program
differences in amino acid loss between high efficiency hemodialysis and postdilution and predilution hemodiafiltration using high convection volume exchange a new metabolic scenario a pilot study
Objective The objective of the study was to quantify the loss of total amino acids (TAAs), nonessential amino acids, essential amino acids, and branched chain amino acids (BCAAs) produced by high-efficiency hemodialysis (HEHD), postdilution hemodiafiltration (HDFpost), and predilution hemodiafiltration (HDFpre) using high ultrafiltration volumes; and to define the specific AA losses registered in HEHD, HDFpost, and HDFpre; to identify a potential metabolic and nutritional decline into protein energy wasting; to compare AA analysis of arterial blood samples taken from healthy controls and patients with end-stage renal disease undergoing hemodialysis. Design and Methods Identical dialysis monitors, membranes, and dialysate/infusate were used to homogenize extracorporeal body influence. Ten patients were recruited and randomized to receive treatment with HEHD, HDFpost, and HDFpre it was used on-line dialytic water methodologies (OL); patients' AA arterial concentrations were measured at the start and on completion of dialysis; TAA from the dialyzer filter was calculated, and baseline levels were subsequently compared with findings obtained 1 year later. Finally, the results obtained were compared with the data from a study of 8 healthy volunteers conducted using bioimpedance analysis and laboratory blood tests to assess nutritional status. Results A higher convective dose results in a higher weekly loss of TAA, nonessential AAs, essential AAs, and BCAAs (HEHD: 15.7 g; HDFpost-OL: 16.1 g; HDFpre-OL: 16.3 g, P P Conclusion The study shows that the AA losses in dialytic liquid are greater after high exchange volume HDF techniques, especially HDFpre. The AA losses are not metabolically compensated, so these increase the derangements of predialytic arterial plasma AA levels. Both AA losses and arterial AA perturbations further worsened body composition already after 12 months of additional dialysis
The strange case of Mr. H. Starting dialysis at 90 years of age: clinical choices impact on ethical decisions.
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