Tetrahydroindoles as Multipurpose Screening Compounds and Novel Sirtuin Inhibitors

Indoles are privileged structures in medicinal and bioorganic chemistry that are particularly well suited to serve as platforms for diversity. Among many other therapeutic areas, the indole scaffold has been used to design aromatic compounds useful to interfere with enzymes engaged in the regulation of substrate acylation status, such as sirtuins. However, the planarity of the indole ring is not necessarily optimal for all target enzymes, especially when functionalization with aromatic side chains is required. Replacement of flat scaffolds by nonplanar molecular cores dominated by sp³ hybridization is a common strategy to avoid the disadvantages associated with poor solubility and high promiscuity, while covering less-well-explored areas of chemical space. Thus, we synthesized fragment-like tetrahydroindoles suitable for fragment-based drug discovery as well as a well-characterized small library intended as multipurpose screening compounds. For proof of principle, these compounds were screened against sirtuins 1–3, enzymes known to be addressable by indoles. We found that 2,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxamides are potent and selective SIRT2 inhibitors. Compound 16 t displayed an IC₅₀ value of 0.98 μm and could serve as exquisite starting point for hit-to-lead profiling.     

Electrocatalytic Reduction of CO2 to Ethylene by Molecular Cu‐Complex Immobilized on Graphitized Mesoporous Carbon

The electrochemical reduction of carbon dioxide (CO₂) to hydrocarbons is a challenging task because of the issues in controlling the efficiency and selectivity of the products. Among the various transition metals, copper has attracted attention as it yields more reduced and C2 products even while using mononuclear copper center as catalysts. In addition, it is found that reversible formation of copper nanoparticle acts as the real catalytically active site for the conversion of CO₂ to reduced products. Here, it is demonstrated that the dinuclear molecular copper complex immobilized over graphitized mesoporous carbon can act as catalysts for the conversion of CO₂ to hydrocarbons (methane and ethylene) up to 60%. Interestingly, high selectivity toward C2 product (40% faradaic efficiency) is achieved by a molecular complex based hybrid material from CO₂ in 0.1 m KCl. In addition, the role of local pH, porous structure, and carbon support in limiting the mass transport to achieve the highly reduced products is demonstrated. Although the spectroscopic analysis of the catalysts exhibits molecular nature of the complex after 2 h bulk electrolysis, morphological study reveals that the newly generated copper cluster is the real active site during the catalytic reactions.     

Decorating surface charge of graphite nanoplate using an electrostatic coupling agent for 3-dimensional polymer nanocomposite

Here, we report a facile approach to electrostatically couple the surface charges of graphite nanoplate (GNP) fillers and poly(methyl methacrylate) (PMMA) polymer particles using ethylene maleic anhydride (EMA) copolymer as an electrostatic coupling agent. Our strategy involved switching the intrinsic repulsive electrostatic interactions between the directly exfoliated GNPs fillers and the PMMA particles to attractive electrostatic surface interactions for preparing core(PMMA)-shell (GNP) precursor in order to optimizing 3-dimensionally dispersed polymer nanocomposite. As a result, the electrical conductivity of the composites dramatically increased by a factor of 16.7 in the EMA-coupled GNP/PMMA composites compared with that of the EMA-free GNP/PMMA composites. In addition, the percolation threshold was also notably reduced from 0.32 to 0.159 vol% after electrostatic coupling of the GNPs fillers and PMMA particles. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020 , 137, 48390.     

Tailoring the electron-blocking layer by addition of YSZ to Ba-containing anode for improvement of ceria-based solid oxide fuel cell

The in-situ fabrication of an electron-blocking layer between the Ba-containing anode and the ceria-based electrolyte is an effective approach in suppressing the internal electronic leakage in ceria-based solid oxide fuel cell (SOFC). To improve the thickness of the electron-blocking layer and to research the effect of the layer thickness on the improvement of SOFC, a Ba-containing compound (0.6NiO-0.4BaZr_0.1Ce_0.7Y_0.2O_3-δ) modified by Y stabilized zirconia (YSZ) was employed as a composite anode in this research. SEM analyses demonstrated that the thickness of the interlayer can be simply controlled by regulating the proportion of YSZ at anode. The in-situ formed interlayer in the cell with the anode modified by 20?mol% YSZ possesses a thickness of 0.9?µm which is more suitable for the cell achieving an enhanced performance.     

复合材料在旋转压缩机上的应用分析

文章介绍了目前旋转式压缩机主要零部件的材料状况,详细论述了金属基复合材料、陶瓷基复合材料在旋转压缩机上的应用情况及前景,为复合材料在压缩机领域的应用提供指导。     

A dense and compact laser cladding layer with solid metallurgical bonding significantly improved corrosion resistance of Mg alloy for engineering applications

Although Mg alloy attracts great attention for engineering applications because of high specific strength and low density, low corrosion resistance limits its extensive use. In this study, Mg–Al–Zn–Mn alloy was treated via a laser cladding process to generate a dense and compact laser cladding layer with solid metallurgical bonding on the substrate for improving corrosion resistance, effectively hindering the corrosion pervasion into Mg alloy. The corrosion current density declined from 103 μA/cm² for Mg alloy to 13 μA/cm² for the laser cladding layer in NaCl aqueous solution. Moreover, the laser cladding layer was slightly corroded in comparison with Mg alloy in NaCl aqueous solution. Besides, the microhardness of the cladding layer reached a mean value of 170.5 HV, 3.1 times of Mg alloy (56.8 HV) due to the in situ formation of hardening intermetallic phases. Wear resistance of laser cladding layer was also obviously improved. These results demonstrated that the laser cladding layer obviously enhanced anticorrosion property of Mg alloy for engineering applications.     

Formation of a protective layer against corrosion on Mg alloy via alkali pretreatment followed by vanillic acid treatment

Although Mg alloy possesses high specific strength, low density, and good biocompatibility, poor corrosion resistance hinders its further applications. In the present study, an innovative protective layer against corrosion was prepared on the AZ31 Mg alloy via alkali pretreatment followed by vanillic acid treatment. The alkali pretreatment supplied –OH for the AZ31 Mg alloy surface to react with vanillic acid. The vanillic acid treatment played a crucial role in enhancing the corrosion resistance due to the excellent ability to act as a barrier and retard aqueous solution penetration, which effectively isolated the underlying Mg alloy from the corrosive environment. The corrosion current density of alkali and vanillic acid-treated Mg alloy (AZ31V) almost showed two orders of magnitude lower values in comparison with that of the AZ31 Mg alloy, and the corrosion potential of AZ31V Mg alloy increased from −1.41 to −1.25 V. The immersion tests proved that there was no occurrence of severe corrosion. Hence, the alkali pretreatment and vanillic acid treatment may represent a promising method to improve the corrosion resistance of Mg alloy.