The NiCoCrAlY alloy with uniform yttrium distribution was fabricated via powder milling and spark plasma sintering. After powder milling, yttrium was uniformly distributed in the alloy in the form of Ni-Y precipitates (50–150 nm) and nano-sized Y2O3 particles (5–30 nm). It was found that the u...

The FTIR and FT-Raman spectra of 1-(m-(trifluoromethyl)phenyl)piperazine [TFMPP] have been recorded in the region 4000–400 cm−1 and 3500–100 cm−1, respectively. The optimized geometry, frequency and intensity of the vibrational bands of the compound was obtained by the density functional theor...

Twenty four new 1-[(4-phenylpiperazin-1-yl)-methyl]- derivatives of 3-phenyl-3-methyl- (6–17) and 3,3-dimethyl-pyrrolidine-2,5-diones (18–29) have been synthesized and evaluated for their anticonvulsant activity in the maximum electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seiz...

The NK1 receptor radioligands 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-4-[11C]methyl-piperazine ([11C]BMP, [11C]1) and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl}-acetic acid [11C]methyl ester ([11C]BME, [11C]2) were synthesized for evaluation as ne...

Separation of monomeric constituents of ethoxylated bisphenol A (BIS-EMA) with between 2 and 15 ethoxy groups per phenol in the molecule was investigated with micellar electrokinetic chromatography at different volume percentages methanol in the background electrolyte (10 mM sodium dodecylsulfat...

Bisphenol A ethoxylate dimethacrylates (Bis-EMA) are transformed into ionisable amines by derivatisation in order to make the analytes applicable to capillary electrophoresis. For this goal, piperidine was added onto the CC double bond of the α,β-unsaturated ester group forming a tertiary am...

IntroductionThe incorporation of light-curable resins has been proposed for mineral trioxide aggregate (MTA) to improve its properties and reduce its setting time. The aim of the present study was to assess the pH and calcium ion release of an experimental bisphenol A ethoxylate dimethacrylate/M...

On the basis of X-ray co-crystal structures of matrix metalloproteinase-13 (MMP-13) in complex with its inhibitors, our structure-based drug design (SBDD) strategy was directed to achieving high affinity through optimal protein–ligand interaction with the unique S1″ hydrophobic specificity poc...

Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences between the histone substrate binding sites in or...

A new series of 4-phenylcoumarin derivatives was synthesized starting from (2-oxo-4-phenyl-2H-chromen-7-yloxy) acetic acid hydrazide 3. Evaluation of the target compounds for their antiviral activity against hepatitis A virus revealed that the ethylthiosemicarbazide derivative 7b was the most po...

Human carbonic anhydrases (hCAs, EC 4.2.1.1) IX and XII are overexpressed in a wide variety of cancers and are considered available drug targets for anti-tumor therapy since their inhibition has been shown to reduce tumor growth and metastasis. A set of coumarin derivatives (1–10) and several 1...

Janus kinases (JAKs) regulate various inflammatory and immune responses and are targets for the treatment of inflammatory and immune diseases. Here we report the discovery and optimization of 1H-pyrazolo[3,4-d]pyrimidin-4-amino as covalent JAK3 inhibitors that exploit a unique cysteine (Cys909) ...

This study represents the synthetic approaches of a new set of 2-(((3-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-4-yl)methylene)hydrazono)-5-(aryl)thiazolidin-4-one derivatives 4–22 aiming to obtain new antiproliferative candidates against human cervix carcinoma cells (Hela) of EGFR PK inhibiting po...

New 4-(2-R-pyrimidin-4-yl)-5-methyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-ones were obtained by reaction of difluoroboron chelate of 4-acetyl-5-hydroxy-3-methyl-1-phenyl-1H-pyrazole with guanidine and its derivatives.

In this work, an enlarged series of 1,2,4-triazolo[4,3-a]pyrazin-3-ones was designed to target the human (h) A2A adenosine receptor (AR) or both hA1 and hA2A ARs. The novel 8-amino-1,2,4-triazolopyrazin-3-one derivatives 1–25 featured a phenyl or a benzyl pendant at position 2 while different a...

Interleukin-2-inducible T-cell kinase (Itk) plays an important role in multiple signal transduction pathways in T and mast cells, and is a potential drug target for treating inflammatory diseases, autoimmune diseases, and T cell leukemia/lymphoma. Herein, we describe the discovery of a series of...

Arene ruthenium(0) complexes with carbonyl side chain functionalities like [Ru(η6-C6H5COR)(η4-COD)] or [Ru(η6-o-C6H4{R1}COR)(η4-COD)] (COD=1,5-cyclooctadiene; R=H, CH3; R1=H, CH3, OCH3) are easily accessible by replacing the naphthalene ligand of [Ru(η6-naphthalene)(η4-COD)] (1) through an...

In the presence of a catalytic amount of TsOH·H2O or TiCl4, 5-silyl-4-pentenoic acids (1), namely vinylsilanes with a carboxy group, were smoothly cyclized to γ-lactones in good to high yields. The difference in the geometry of the carboncarbon double-bond did not affect the reaction rate. T...

The typical properties and yield of the refined hydrothermolytic acid (RHTA) and refined hydrothermolytic oxidation acid (RHOA) respectively prepared from cotton stalk by the hydrothermolysis process with and without hydrogen peroxide at 180–280 °C were investigated. The pH of RHOA at 180–260...

Bond angles at thiohydroxamate oxygen in crystal structures of 3-alkoxy-5-(p-methoxyphenyl)-4-methylthiazole-2(3H)-thiones gradually increased with the size of the 3-alkoxy substituent. This effect was attributed to strain on the basis of (i) a linear free energy relationship (Taft–Dubois corre...