2-Phenyloxazole-4-carboxamide as a Scaffold for Selective Inhibition of Human Monoamine Oxidase B

A series of 2-phenyloxazoles bearing an amide group at position 4 were designed and synthesized for evaluation as potential inhibitors of human recombinant monoamine oxidases (hrMAOs). Results of kinetics experiments demonstrated that all compounds behave as competitive MAO inhibitors, with good selectivity toward the MAO-B isoform. The most potent and selective derivatives are characterized by inhibition constant (K_i) values in the sub-micromolar range and a good selectivity index (K_{i MAO-A}/K_{i MAO-B}>50). Some derivatives were also found to be able to inhibit MAO activity in nerve growth factor (NGF)-differentiated PC12 cells, taken as a model of neuronal cells. In particular, 2-(2-hydroxyphenyl)-N-phenyloxazole-4-carboxamide (compound 4 a ) may be a promising new scaffold, exerting the highest selectivity and inhibitory effect toward MAOs in NGF-differentiated PC12 cell lysates, without compromising cell viability. Molecular docking analysis allowed a rationalization of the experimentally observed binding affinity and selectivity.     

Decorative near-infrared transmission filters featuring high-efficiency and angular-insensitivity employing 1D photonic crystals

We present a new scheme for visibly-opaque but near-infrared-transmitting filters involving 7 layers based on one-dimensional ternary photonic crystals, with capabilities in reaching nearly 100% transmission efficiency in the near-infrared region. Different decorative reflection colors can be created by adding additional three layers while maintaining the near-infrared transmission performance. In addition, our proposed structural colors show great angular insensitivity up to ±60° for both transverse electric and transverse magnetic polarizations, which are highly desired in various fields. The facile strategy described here involves a simple deposition method for the fabrication, thereby having great potential in diverse applications such as image sensors, anti-counterfeit tag, and optical measurement systems.

     

Production technology for low-carbon,low-sulfur boron steel

A technology for slag formation in the ladle–furnace unit is considered; the slag is based on the CaO–SiO₂–MgO–Al₂O₃–B₂O₃ system. This technology permits both microalloying of the steel with boron (reduced from the oxide phase) and desulfurization of the steel. The resulting boron content in the steel is 0.001–0.008%; the sulfur content in low-alloy steel and pipe steel is low (0.004–0.010%); and the consumption of manganese ferroalloys is reduced to 0.5 kg/t for 08кп steel and 1.4 kg/t for 09Г2C steel. In addition, the proposed technology increases the strength of the rolled steel, without loss in its plasticity; and reduces the environmental impact thanks to the replacement of fluorspar by colemanite.     

Ga-doped IZO films obtained by magnetron sputtering as transparent conductors for visible and solar applications

C-axis textured thin films of gallium-doped indium zinc oxide (GIZO) with a 2% ratio of Ga/Zn, were obtained via RF-magnetron sputtering with high transparency and electrical conductivity. A Box-Behnken response surface design was used to evaluate the effects of the deposition parameters (In₂O₃ target power, deposition time, and substrate temperature) on the chemical composition, optical, electrical, and structural properties of the GIZO films. The optical constants and the electrical properties were obtained using optical models. The GIZO stoichiometry, and therefore the In/Zn atomic ratio, affected the crystallinity, crystalline parameters, band gap, and charge carrier mobility of the GIZO films. The charge carrier density was related to the change in the crystalline parameters of the hexagonal structure and the In/Zn atomic ratio. The best electrical conductivity values (1.75?×?10³ Ω^?1 cm^?1) were obtained for GIZO films with In/Zn ratio ≥?1. Several figures of merit (FOM) defined for the visible and solar regions were comparatively used to select the optimal In/Zn atomic ratio that provided the best balance between the conductivity and the transparency. The optimal In/Zn ratio was in a range of 0.85–0.90 for the GIZO films.     

Method for Constructing Periodic Solutions of a Controlled Dynamic System with a Cylindrical Phase Space

Journal of Computer and Systems Sciences International - We consider a controlled mechanical system with one degree of freedom described by an angular coordinate. The system is under the action of...     

基于状态空间法的电动机故障诊断和识别

电动机的初期故障信号一般较弱,不易辨别,而状态空间法在小信号的处理中灵敏度很高。为达到对电动机故障的诊断和识别,试图把状态空间法应用到对电动机的故障诊断中,先通过推导,从数学理论层面分析了状态空间法对于电动机故障信号的可辨别性,再使用Matlab软件搭建状态空间的辨别模型,把实验台测试的三组数据导入到模型中进行测试。测试的结果有力地证明了此方法的可行性,并能克服快速傅里叶变换(FFT)中数据采集量较大、分辨率不高的缺点。     

A Dual Inhibitor of DYRK1A and GSK3β for β-Cell Proliferation: Aminopyrazine Derivative GNF4877

Loss of β-cell mass and function can lead to insufficient insulin levels and ultimately to hyperglycemia and diabetes mellitus. The mainstream treatment approach involves regulation of insulin levels; however, approaches intended to increase β-cell mass are less developed. Promoting β-cell proliferation with low-molecular-weight inhibitors of dual-specificity tyrosine-regulated kinase 1A (DYRK1A) offers the potential to treat diabetes with oral therapies by restoring β-cell mass, insulin content and glycemic control. GNF4877, a potent dual inhibitor of DYRK1A and glycogen synthase kinase 3β (GSK3β) was previously reported to induce primary human β-cell proliferation in vitro and in vivo. Herein, we describe the lead optimization that lead to the identification of GNF4877 from an aminopyrazine hit identified in a phenotypic high-throughput screening campaign measuring β-cell proliferation.