No abstract is provided for this article.
Background: Butyrylcholinesterase (BChE) is known serine hydrolase enzymes responsible for the hydrolysis of acetylcholine (ACh). Although the role of the other serine hydrolase enzyme, acetylcholinesterase (AChE) in cholinergic transmission is well known, the role of BChE has not been elucidated sufficiently. The hydrolysis of acetylcholine in the synaptic healthy brain cells mainly carried out by AChE, it is accepted that contribution to the hydrolysis of BChE is very low; but both AChE and BChE are known to play an active role in neuronal development and cholinergic transmission. Docking is a method that predicts the preferential orientation of a molecule (small molecule) to a second (protein) molecule when connected to form a stable complex. It is used to predict the affinity of small molecule drug candidates against protein targets, their binding to these proteins, and hence their biological activity. Objective: In this study, we examined a series of pyridazinone-derived compounds, previously synthesized by our research group, for the compatibility of BChE enzyme and some physicochemical properties of the compounds <i>in silico</i>. Method: The compounds were optimized by conjugated gradient method by creating three dimensional models with OPLS_2005 force field parameters with 2D Sketcher and MacroModel (Schrödinger, LLC, NY) software in Maestro (Schrödinger, LLC, NY). Results: When the activities of the compounds were compared with the physicochemical parameters calculated by computerized methods, some parameters were found to be directly related to the activity. Conclusion: This study supports that the researchers may use to calculate various physicochemical properties and to make molecular modeling studies before working with pyridazinone derivates.
Abstract Ferrochrome slag (FS) and ground granulated blast furnace slag (GGBFS) were used as resource material in geopolymer concrete mixtures. A mixture of 10 M sodium hydroxide (NaOH) and sodium silicate (Na 2 SiO 3 ) was used as the activator. After the two different slag‐based geopolymer concrete (SGC) mixtures were prepared and molded. They were kept at 80°C for 24 hr, and then the SGC samples were cured in 23 ± 1°C water for 27 days. Samples that completed the curing times were exposed to the 300 freeze–thaw (F–T) cycles. The compressive strength, ultrasonic pulse velocity, relative dynamic elasticity modulus values, weight changes, and appearances of the SGC samples were examined at the end of every 50 F–T cycles. Scanning electron microscopy analysis was performed to examine the microstructure changes of the samples after 300 F–T cycles. As the GGBFS proportion in the SGC mix increased, the mechanical properties of the samples against the F–T effect increased. Samples containing 100% FS and 75% FS fell apart at the end of 150 and 200 F–T cycles, respectively. The deterioration of the geopolymer gel structures of the samples exposed to F–T was decreased with increasing GGBFS ratio in the mix.
Turkey is located on a seismically active region. The active fault zones, primarily the North Anatolian Fault and East Anatolian Fault, constitute a center to the movements. On 24 January 2020 at local time 20:55, an earthquake of Mw = 6.8 struck Sivrice, Elazığ located in eastern part of Turkey. After this main shock, 1185 aftershocks were recorded until February 8, 2020. The main event resulted in 41 human casualties and 1632 injured. Also, 45 people were salvaged from the debris. The earthquake mostly affected to Elazığ and Malatya provinces. 633 buildings were demolished, 10492 buildings were severely damaged, 2161 buildings were moderately damaged, and 16046 buildings were slightly damaged in the affected region. This paper focus on evaluating the damages and failures of masonry, adobe, and historical structures in the affected areas around Elazığ and Malatya provinces.
Aim: The aim of this study is to provide a qualitative and quantitative explanation of the structure activity relationships with pharmacophore analysis and Quantitative Structure Activity Relationship (QSAR) studies of the compounds synthesized as acetylcholinesterase enzyme inhibitor by our research group. Material and Methods: Maestro 11.9 (Schrodinger, New York) was used for pharmacophore model studies. Pharmacophore analysis was performed for all compounds showing acetylcholine esterase inhibitory effect. For QSAR studies, various physicochemical parameters of these compounds were calculated using GaussView 5.0 and ChemDraw 15.0 programs. Regression analysis was performed by using these parameters and QSAR equation was obtained. Results: All compounds overlapped and hypotheses generated. The most appropriate pharmacophore model was created by comparing the hypothesis and activity results of the compounds. The analyses were performed using 8 different parameters for all compounds. R2 value of equation was found 1. Conclusion: The pharmacophore analysis and the QSAR equation are applicable for all compounds synthesized as acetylcholinasterase inhibitory and containing pyridazinon-2-ylacetohydrazide structure. Also, the estimated IC50 values can be calculated before the compounds are synthesized using the QSAR equation.
concrete strength levels, namely, of 25 and 40 MPa. Load-displacement curves, energy absorption capacities, stiffness degradation, the moment-curvature relationship, the plastic hinge mechanism and the ductility index were experimentally obtained at two different concrete types along with the measured stress-strain properties of the conventional and perlite concrete. The test results showed that the construction of the RC columns using only perlite may become possible in future by providing an adequate concrete stress-strain capacity, which will be improved.
Objective: Anemia commonly accompanies chronic kidney disease (CKD). Erythropoiesis-stimulating agents (ESAs), such as darbepoetin, are initiated for anemia in CKD. Additionally, hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitors have demonstrated efficacy in treating CKD-associated anemia. This meta-analysis aims to compare the efficacy, safety, and tolerability of enarodustat in anemic CKD patients.Case report Methodology: A systematic search of Cochrane CENTRAL, Ovid Medline R, PubMed, and Web of Science databases up to March 1, 2024, was conducted. Randomized controlled trials (RCTs) directly comparing enarodustat with darbepoetin were included. Data from four unique RCTs comprising an inverse variance-weighted random-effects model were utilized for the main analysis. Primary efficacy outcome measures included hemoglobin (Hb) change at weeks 4-6 and during follow-up, while primary safety outcomes focused on serious adverse events (SAEs). Subgroup analyses were performed based on dialysis status and prior use of ESA for the primary outcome. Results: Four RCTs with 7 reports involving 586 patients were included in the main analysis. Enarodustat demonstrated superiority to control in terms of change in Hb levels at week 4-6 (RR 0.76, 95% CI 0.02 to 1.50, I2=96%, p=0.04) but non-inferiority during follow-up (MD 0.66, 95% CI -0.22 to 1.53, I2=91%, p=0.14). Enarodustat exhibited comparable effects for safety and tolerability parameters such as SAEs (RR 1.17, 95% CI 0.72 to 1.91, I2=0%, p=0.52), any adverse events (RR 0.95, 95% CI 0.82 to 1.08), any adverse events leading to discontinuation (RR 0.90, 95% CI 0.37 to 2.20), diarrhea (RR 1.50, 95% CI 0.05 to 43.15), hypertension (RR 0.89, 95% CI 0.43 to 1.84), and all-cause mortality (RR 0.63, 95% CI 0.08 to 5.08). Subgroup analysis by dialysis status revealed nonsignificant differences for change in Hb levels at week 4-6 and during follow-up, but comparator-based subgroup analysis demonstrated a significant difference only when comparing to placebo at week 4-6. Conclusion: Enarodustat exhibits promise as a treatment option for anemia associated with CKD, demonstrating superiority to control in terms of Hb change at week 4-6 and non-inferiority during follow-up. Moreover, it demonstrates comparable safety and tolerability profiles to darbepoetin, making it a potential alternative in the management of CKD-related anemia.
I
 n this study, four new oxime ether derivatives were synthesized and their antimicrobial activities were evaluated. At the
 same time, a comparison of the efficiency of the conventional method of synthesis with the microwave method was investigated. The structures of synthesized compounds were confirmed by their IR, 1H-NMR, and HRMS spectra. Antimicrobial
 activity of the compounds was tested against two Gr (+) bacteria (S. aureus, E. faecalis), two Gr (-) bacteria (P. aeruginosa, E.
 coli), and three yeast-like fungi (C. albicans, C. krusei, C. parapsilosis) by modified agar dilution method.
Recently, geopolymer binders have the popularity they deserve in terms of the effort spent on them, as they provide the opportunity to produce high-performance and eco-friendly composites by minimizing the environmental and durability problems caused by cement production and usage. This study was designed to examine the effects of different ratios of waste rubber fiber (WRF) replaced with coarse aggregate on the performance of geopolymer concrete (GPC) samples. The binder part was obtained by substituting 2% nano silica to the granulated blast furnace slag (GBFS). Additionally, in this study, in which natural river sand was used as fine aggregate, WRF substitution was applied to coarse aggregate at different ratios (0%, 5%, 10% and 15%). Following the solid part of GPC samples was obtained as described, the alkaline activation was provided using a 12 M NaOH solution. At the end of 28-day curing period, compressive strength, flexural strength, splitting tensile strength, impact resistance, capillary permeability and elevated temperature performance properties were investigated in detail. Furthermore, the obtained experimental findings were interpreted with microstructural analysis. The results showed that the usage of WRF improved properties such as flexural strength, tensile strength, impact resistance, and also had a negative effect on compressive strength.
No abstract is provided for this article.
No abstract is provided for this article.
Nafimidone and nafimidone alcohol, which were synthesized in 1981 and whose anticonvulsant activities were determined, are important anticonvulsant compounds in the structure of (arylalkyl)azole, which reached the stage of clinical human studies but could not pass this stage. In this study, the commercially available chiral stationary phase amylose tris(3,5-dimethyphenylcarbamate) (Chiralpak AD) was used to establish direct enantiomeric separations of nafimidone alcohol which is the methabolite of nafimidone in the normal phase HPLC mode. Investigations were also done into the compositional influences of the mobile phase. When the mobile phase was switched from methanol to n-hexane, the retention times were shortened. The mobile phase of methanol/n-hexane (70:30 v/v) at a flow rate of 0.2 mL/min produced the best results, with an enantiomer resolution of 0.83. Consequently, further chemical and pharmacological research on nafimidone alcohol and its enantiomers can be facilitated by the proposed HPLC approach.
Abstract In this study, mechanical, visual, and microstructure changes of geopolymer concrete exposed to sulfate and salt effects were investigated. Elazığ ferrochrome slag (EFS) and blast furnace slag (BFS)‐based geopolymer concretes which completed curing time were immersed in 5% sodium sulfate (Na 2 SO 4 ), magnesium sulfate (MgSO 4 ), sodium chloride (NaCl), and magnesium chloride (MgCl 2 ) solutions for 12 weeks. The compressive strength values, ultrasonic pulse velocities, visual inspections, weight, and length changes of the samples were determined in this investigation. In addition, scanning electron microscopy was performed for the microstructure analysis of the samples removed from the solutions. Sulfate solutions had a more negative effect on the samples than salt solutions. As the EFS ratio in the mixture increases, the loss rate in the strength of the samples exposed to sulfate and salt solutions decreased. While samples exposed to sodium chloride, sodium sulfate, and magnesium sulfate solutions occurred weight gain, samples exposed to magnesium chloride occurred weight loss. The samples in salt solutions shrank, while the samples in sulfate solutions expanded. No deterioration occurred on the surfaces of the samples exposed to the solutions for 12 weeks.
