BMS Derivatives C7-Linked to β-Cyclodextrin and Hyperbranched Polyglycerol Retain Activity against R5-HIV-1NLAD8 Isolates and Can Be Deemed Potential Microbicides

Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring. These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions. Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5-HIV-1_NLAD8 isolates. Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4^th generation, are reported here for the first time.     

High temperature tribological characterisation of TiAlSiN coatings produced by cathodic arc evaporation

This study reports on the wear properties at medium-high temperatures of TiAlSiN films deposited by cathodic arc evaporation on hot work steel substrates. The chemical composition and microstructure of the coatings were characterised by glow discharge optical emission spectroscopy, scanning electron microscopy and X-ray diffraction. The mechanical properties, i.e. hardness and elastic modulus were evaluated by nanoindentation, and the adhesion of the coatings was tested by scratch tests. Coatings with stoichiometries of Ti_0.31Al_0.1Si_0.06N_0.53 and Ti_0.23Al_0.12Si_0.09N_0.55 exhibit microstructures consisting of solid solutions of (Ti,Al,Si)N, where Al and Si replace Ti atoms. These films show high hardness and good adhesion strength to the hot work steels. Conversely, coatings with a stoichiometry of Ti_0.09Al_0.34Si_0.02N_0.55 show a wurtzite-like microstructure, low hardness and poor adhesion strength.The wear rates of the coatings were investigated by ball-on-disc experiments at room temperature, 200 °C, 400 °C and 600 °C, using alumina balls as counter surfaces. At room temperature, the films show wear rates of the same order of magnitude of TiN and TiAlN coatings. On the other hand, the wear rates of solid solution (Ti,Al,Si)N coatings measured at 200, and 400 °C are one order of magnitude smaller than those measured at room temperature due to the formation of oxide-containing tribofilms on the wear tracks. At 600 °C the wear rates increase but still keep smaller than those measured at room temperature, although this effect can be influenced by the softening of the steel substrates by over-tempering. EDS analyses revealed that, between 200 °C and 400 °C, the oxidation of the coating occurs only at the contact zone between the film and the counterpart body due to the sliding process.     

Improved thermal stability of oxide-supported naked gold nanoparticles by ligand-assisted pinning

We report a method to improve the thermal stability, up to 900 °C, of bare-metal (naked) gold nanoparticles supported on top of SiO(2) and SrTiO(3) substrates via ligand-assisted pinning. This approach leads to monodisperse naked gold nanoparticles without significant sintering after thermal annealing in air at 900 °C. The ligand-assisted pinning mechanism is described.     

A multiscale parallel computing architecture for automated segmentation of the brain connectome

Several groups in neurobiology have embarked into deciphering the brain circuitry using large-scale imaging of a mouse brain and manual tracing of the connections between neurons. Creating a graph of the brain circuitry, also called a connectome, could have a huge impact on the understanding of neurodegenerative diseases such as Alzheimer's disease. Although considerably smaller than a human brain, a mouse brain already exhibits one billion connections and manually tracing the connectome of a mouse brain can only be achieved partially. This paper proposes to scale up the tracing by using automated image segmentation and a parallel computing approach designed for domain experts. We explain the design decisions behind our parallel approach and we present our results for the segmentation of the vasculature and the cell nuclei, which have been obtained without any manual intervention.     

Polycarbonate films metalized with a single component molecular conductor suited to strain and stress sensing applications

The paper reports all-organic strain and stress sensitive films that use electrical monitoring approach. The films were prepared by self-metallizing polycarbonate films with the single component molecular conductor [Au(α-tpdt)₂]⁰ (tpdt = 2,3-thiophenedithiolate). It was shown that [Au(α-tpdt)₂]⁰ by its nature is able to form metallic solid material with low crystallinity. Electromechanical tests demonstrated that the developed films are strain-resistive materials with advanced elastic properties: their electrical resistance varies linearly with uniaxial elongation up to relative strain being of 1.0% that is about five times larger than that for conventional metals. The gauge factor of the films is 4.4 and stress sensitivity is 30 Ω/bar. The processing characteristics of polycarbonate films, self-metalized with a metallic [Au(α-tpdt)₂]⁰-based layer, make them potentially useful for engineering flexible, lightweight, strain and pressure sensors. Due to electromechanical characteristics these films are suited to strain sensing applications requiring miniature strain control in a wide deformation range.     

西班牙毛革两用服装革加工理论及工艺技术应用

通过系统介绍具有国际领先水平的西班牙毛革两用服装革的加工原理及工艺技术应用 ,具体阐明了其漫长而复杂的生产流程 ,以及每道工序应如何做和这样做的理论依据。强调以绵羊皮为原料加工生产毛革两用服装革鞣制前脱脂的重要性。只有前期好的脱脂 ,才有好的鞣制 ,最终才有所要的理想的各种产品风格。     

西班牙毛革两用服装革加工理论及工艺技术应用(续)

通过系统介绍具有国际领先水平的西班牙毛革两用服装革的加工原理及工艺技术应用 ,具体阐明了其漫长而复杂的生产流程 ,以及每道工序应如何做和这样做的理论依据。强调以绵羊皮为原料加工生产毛革两用服装革鞣制前脱脂的重要性。只有前期好的脱脂 ,才有好的鞣制 ,最终才有所要的理想的各种产品风格。     

Key role of the resin layer thickness in the lability of complexes measured by DGT

Analysis of the dynamic features of diffusion gradients in thin film devices (DGT) indicates that the penetration of complexes into the resin layer dramatically increases their lability. This should be taken into account when interpreting DGT measurements in terms of the dynamics of solution speciation. The experimental accumulation of Cd by DGT sensors in Cd-NTA systems confirmed these theoretical analyses. A computational code, which allows a rigorous digital simulation of the diffusion-reaction processes in the gel and resin layers, was used to model the results and to demonstrate the effect of the complex penetration into the resin layer on the lability degree. These findings suggest that DGT renders all complexes much more labile than if the resin-diffusive gel interface was considered as a perfect planar sink, explaining why DGT often measures a high proportion of the metal in a natural water. This information is relevant since some studies have stressed the importance of labile complexes as a source of bioaccumulated metal.