[2.2]Paracyclophane-Based TCN-201 Analogs as GluN2A-Selective NMDA Receptor Antagonists

Recent studies have shown the involvement of GluN2A subunit-containing NMDA receptors in various neurological and pathological disorders. In the X-ray crystal structure, TCN-201 ( 1 ) and analogous pyrazine derivatives 2 and 3 adopt a U-shape (hairpin) conformation within the binding site formed by the ligand binding domains of the GluN1 and GluN2A subunits. In order to mimic the resulting π/π-interactions of two aromatic rings in the binding site, a [2.2]paracyclophane system was designed to lock these aromatic rings in a parallel orientation. Acylation of [2.2]paracyclophane ( 5 ) with oxalyl chloride and chloroacetyl chloride and subsequent transformations led to the oxalamide 7 , triazole 10 and benzamides 12 . The GluN2A inhibitory activities of the paracyclophane derivatives were tested with two-electrode voltage clamp electrophysiology using Xenopus laevis oocytes expressing selectively functional NMDA receptors with GluN2A subunit. The o-iodobenzamide 12 b with the highest similarity to TCN-201 showed the highest GuN2A inhibitory activity of this series of compounds. At a concentration of 10 μM, 12 b reached 36 % of the inhibitory activity of TCN-201 ( 1 ). This result indicates that the [2.2]paracyclophane system is well accepted by the TCN-201 binding site.     

Primary Study of a Settling Fiber Particle in a Particle Cloud

Fiber particles have some unique behaviors due to their special shapes, which are important to those related industries. When a single fiber is in a particle cloud, its behavior will be influenced by others around it. Hence, the behavior of an isolated fiber particle will be different from that in a particle cloud, such as aggregation, orientation, and drag coefficient. However, little information is available on these phenomena, especially drag coefficient. Therefore, this article focuses on the settling process of a fiber particle in a particle cloud. Experiments were conducted to observe the settling behavior of fiber particles and to determine the drag coefficients of an isolated fiber particle in a particle cloud. The relationship between drag coefficient, orientation, and Re for different fiber particles is obtained, which is independent of volume concentration. It is further observed that the aspect ratio has little influence on the drag coefficients of fiber particles. By comparison, it is noticed that these relationships are similar to those found for an isolated single-fiber particle. Furthermore, the orientation of a fiber particle in a particle cloud fluctuates around the stable horizontal orientation in the same way as a single-fiber particle, but returns to the steady state more quickly.     

Hydrothermal synthesis of carbonate-free submicron-sized barium titanate from an amorphous precursor: Synthesis and characterization

In this paper, the amorphous barium titanate precursor was prepared by the peroxo-hydroxide method and post-treated by various drying procedures, such as: room temperature drying, room temperature vacuum drying and vacuum drying at 50 °C. The objective in the latter two treatments was to increase the Ti-O-Ba bonds of the precursor. The post-treated precursors were compared with the untreated (i.e., ‘wet’) precursor. Also, a barium titanate precursor was prepared by an alkoxide route. Afterwards, the precursors were hydrothermally treated at 200 °C in a 10 M NaOH solution. Vacuum drying of the precursor seemingly promoted the formation of Ti-O-Ti bonds in the hydrothermal end-product. The low Ba:Ti ratio (0.66) of the alkoxide-route prepared precursor lead to a multi-phase hydrothermal product with BaTiO₃ as the main phase. In contrast, phase pure BaTiO₃, i.e. without BaCO₃ contamination, was obtained for the precursor which was dried at room temperature. Cube-shaped and highly crystalline BaTiO₃ particles were observed by electron microscopy for the hydrothermally treated peroxo-hydroxide-route prepared precursor.     

Elimination of drift-like errors in intelligent cyclic A/D converters

The paper presents a new method of elimination of influence of drift-like errors in so called intelligent cyclic A/D converters, in particular, errors caused by drifts (droops) of voltage at the output of sample-and-hold blocks. The method is based on application of the extended multi-dimensional algorithm, which estimates simultaneously values of the input sample and drift rate. Implementation of the extended algorithm in the intelligent cyclic A/D converters requires only insignificant changes in the digital part of the converter and does not increase their production costs. The motivations to these investigations resulted from practical realizations of the intelligent cyclic A/D converter in CMOS technology and difficulties in design of a precise sample-and-hold circuit. The results of selected simulation experiments related to analysis of influence of a droop rate on the final performance of the intelligent cyclic A/D converters employing the standard (one-dimensional) and extended algorithms are discussed and compared in the paper. The results of experiments show that application of the proposed solution enables efficient functioning of the converters even in the presence of relatively large drifts.     

Synthesis and phase stability of precursor derived HfO2/Si-C-N-O nanocomposites

Hafnium alkoxide modified polysilazane was synthesized by the drop-wise addition of hafnium tetra(n-butoxide) to polysilazane. The solid state thermolysis (SST) temperature and the ceramic yield for both the polysilazane and modified polysilazane were determined by performing thermogravimetry. Fourier transform infrared spectroscopy was performed to understand the polymer to ceramic conversion as well as the bonding characteristics of the ceramics. The modified polymer after crosslinking was subjected to SST at 800 °C at a constant heating rate of 5 °C/min for a dwell time of 2 h in atmospheric ambience. From the X-ray diffractograms, the as-thermolysed ceramics were observed to remain X-ray amorphous and on heat-treatment resulted in the crystallization of tetragonal hafnia. However, on heat-treatment at 1500 °C, reverse phase transformation from tetragonal to monoclinic hafnia was observed. Raman spectroscopy and transmission electron microscopy were employed to further understand the phase evolution. The thermal stability and the influence of amorphous matrix on the coarsening of HfO₂ were also evaluated.     

Numerical study of the effects of reinforcement/matrix interphase on stress-strain behavior of YAl2 particle reinforced MgLiAl composites

For the potential influence produced by the reinforcement/matrix interphase in particle reinforced metal matrix composites (PMMCs), a unit cell model with transition interphase was proposed. Uniaxial tensile loading was simulated and the stress/strain behavior was predicted. The results show that a transition interphase with both appropriate strength and thickness could affect the failure mode, reduce the stress concentration, and enhance the maximum strain value of the composite.     

Defect-free MoS2 nanosheets: Advanced nanofillers for polymer nanocomposites

The preparation of defect-free MoS₂ nanosheets is a key challenge and essential for practical applications. Herein the dodecanethiol was firstly performed as the antioxidant and surface modifier to produce the defect-free MoS₂ by direct ultrasonication of bulk MoS₂ in N,N-dimethylformamide. Incorporating defect-free MoS₂ into polyethylene obviously improved the properties of PE/MoS₂ nanocomposites. For crystallization under quiescent condition, the half crystallization time (t₀.₅) of nanocomposites containing 0.2 wt% MoS₂ was reduced by 87.0% compared to that of neat PE. A 54.3 °C increase in the temperature of maximum weight loss (T_max) was observed by inclusion of as low as 0.7 wt% defect-free MoS₂ nanosheets. In addition, the uniformly distributed MoS₂ can considerably improve the mechanical properties of composites. These observations suggest that the robust nature, dramatic barrier action of defect-free MoS₂ and the strong nanosheets/matrix interfacial adhesion would be the motivation to improve the performance of the polymeric nanocomposites.     

Synthesis of porous silicon nitride using silica/carbon composite derived from phenol–resorcinol–formaldehyde gel

Mesoporous silicon nitride (Si₃N₄), which is one of the most promising structural materials for applications in high-temperature filtration, was synthesized from the carbothermal reduction and nitridation of a pyrolyzed silica-containing phenol-resorcinol-formaldehyde (PRF) gel. The PRF gel was synthesized by combining sol–gel and polymerization of phenol, resorcinol and formaldehyde using sodium carbonate as a catalyst. Silica was incorporated into the gel by addition of 3-aminopropyl trimethoxysilane (APTMS) as a silica precursor. After aging and being freeze-dried, the silica/PRF composite was pyrolyzed under nitrogen gas to convert it into porous silica/carbon composite. The combination of phenol-formaldehyde (PF) and resorcinol-formaldehyde (RF) gels into PRF gel, allows further enhancement in porosity of the silica/carbon composite via pre-calcination in the range of 400–500 °C, since carbon derived from PF gel and that from RF gel have different thermal stability. The final product obtained after final calcination to remove residual carbon has a surface area as high as 194 m²/g, which is significantly much higher than the conventional Si₃N₄ granules. Specific surface area of the product is affected by molar ratio of phenol-to-resorcinol, molar ratio of silica-to-carbon, and the pre-calcination temperature.     

Damage in biocomposites: Stiffness evolution of aligned plant fibre composites during monotonic and cyclic fatigue loading

The non-linear stress–strain behaviour of plant fibre composites is well-known in the scientific community. Yet, the important consequences of this, in terms of the evolution of stiffness as a function of applied strain and cycles to failure, are not well-studied in literature. This is despite the fact that stiffness degradation is a well-accepted indicator of damage in a composite material, and is regularly used as a component failure criterion. This article systematically explores the evolution of stiffness of various aligned plant fibre composites, subjected to (i) monotonic loading, (ii) low-cycle, repeated progressive loading, and (iii) fatigue loading. The evolution in stiffness in plant fibre composites is found to be complex: structural changes in the elementary fibre cell wall and damage development in the composite have often competing effects on stress–strain behaviour. Indeed, the evolution in stiffness of plant fibre composites is found to be unlike that typically observed in traditional composites, and therefore needs to be taken into account in the design of structural components.     

Synthesis at several length scales of zeolite A membranes using a continuous flow method

Zeolite A membranes were synthesized in the inner side of porous TiO₂ and α-Al₂O₃ tubular supports by a continuous method. The methodology was then used at several scales for preparing membranes on TiO₂ and α-Al₂O₃ supports with lengths of 6, 12 and 25 cm. Formation of an homogeneous zeolite film was confirmed by XRD and SEM in all supports. Single-gas permeation experiments (He, H₂, N₂ and n-C₃H₈) indicated that Knudsen diffusion was the predominant mechanism in both supports. All the synthesized membranes present high flux and moderate selectivity to water in water–ethanol mixtures.