Identification and Optimization of 4‐Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase

4‐Anilinoquinolines were identified as potent and narrow‐spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4‐anilino group and the 6,7‐quinoline substituents produced GAK inhibitors with nanomolar activity, over 50 000‐fold selectivity relative to other members of the numb‐associated kinase (NAK) subfamily, and a compound (6,7‐dimethoxy‐N‐(3,4,5‐trimethoxyphenyl)quinolin‐4‐amine; 49 ) with a narrow‐spectrum kinome profile. These compounds may be useful tools to explore the therapeutic potential of GAK in prevention of a broad range of infectious and systemic diseases.     

A Cubic Silsesquioxane Chemically Modified with a PAMAM Dendrimer G0: an Application in Electro-Oxidation of Ascorbic Acid

Silicon - Octa-(3-chloropropyl) octasilsesquioxane (SS) was functionalized with a PAMAM dendrimer (SP) and characterized by some spectroscopic techniques such as Fourier Transform Infrared, Nuclear...     

Analysis of the drying process of a biopolymer (poly-hydroxybutyrate) in rotating-pulsed fluidized bed

A rotating-pulsed fluidized bed (RPFB) dryer was employed to conduct the drying of poly-hydroxybutyrate (PHB) cohesive granules. Along the experiments, it was possible to identify, visually, 3 different dynamic regimes that were related with the temperature profile, the drying kinetics and the fluid dynamic behavior. The drying kinetics of PHB showed a short constant drying rate period followed by a decreasing drying rate period. The constant drying rate (N_c) and final moisture content (dry basis) were related to the rotation frequency (responsible for the pulsation effect), temperature and velocity of the inlet air. Furthermore, measurements of molecular mass (gel permeation chromatography analysis) and Carr Index (flowability test) on PHB samples were done before and after the drying. The RPFB dryer showed to be appropriate to dry the PHB granules, resulting in an excellent fluid dynamic behavior that provided uniform drying of the solid. The best conditions of drying were identified at 7 Hz of rotation frequency, 90 °C and 0.55 m/s of inlet air temperature and velocity. At these conditions the dried PHB reached final moisture content of 0.56% (wet basis) after 2 h of drying.     

Investigation of nanovesicle liposome powder production from soy lecithin by spray drying

ABSTRACT

Aiming to produce stable nanosize liposome vesicles (～100?nm), in a powder form, this study investigated the use of combined microfluidization–spray drying processes, using lactose as a stabilizing agent for vesicles during the process of dehydration. To determine the effective amount of lactose for stabilization, the vesicles were prepared at three different ratios (1:1, 1:3, and 1:5) of lecithin:lactose. The physicochemical properties of the nanoliposome powder and its reconstituted solution with water were evaluated over a storage period of 90 days at water activity below 0.3. The results demonstrated that upon addition of appropriate amount of lactose (1:3 or 1:5 of lecithin:lactose ratio), the aggregation of nanoliposomes was prevented and their size was maintained at lower than 130?nm during storage. Peroxide values of all nanoliposome formulations during the storage period remained below 3?meq/kg and there was no change in L*, a*, b* color parameters. The X-ray photoelectron spectroscopy analysis showed over-representation of lecithin on the power particle surface as compared to the bulk composition.     

Alloys and oxides on carbon-supported Pt-Sn electrocatalysts for ethanol oxidation

This work reports studies of ethanol oxidation on Pt-Sn/C catalysts with nearly the same particle size and identical overall composition having different amounts of oxide and alloyed phases. Results of characterization of physical properties by transmission electron microscopy (TEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC), X-ray photoelectron spectroscopy (XPS), and in situ dispersive X-ray absorption spectroscopy (DXAS) are presented. The variation in the amount of oxide and alloyed phases, promoted by heat treatments in mild temperature conditions, does not produce any significant particle growth. Cyclic voltammetry and oxidation of adsorbed CO in acid medium are used to probe the surface conditions. Data on the electrocatalytic activity towards ethanol oxidation, obtained by potential sweeps and chronoamperometry, are discussed and correlate well with the physical properties. This study, carried out in the absence of composition and particle size effects, shows that the electrocatalytic activity towards ethanol oxidation is strongly influenced by the changes in the amounts of Sn in alloyed and oxidized forms, and that the increase in the amount of alloy at expense of the oxides improves the catalytic activity.     

Adsorption of Cd2+ on carboxyl-terminated superparamagnetic iron oxide nanoparticles

The affinity of Cd(2+) toward carboxyl-terminated species covalently bound to monodisperse superparamagnetic iron oxide nanoparticles, Fe(3)O(4)(np)-COOH, was investigated in situ in aqueous electrolytes using rotating disk electrode techniques. Strong evidence that the presence of dispersed Fe(3)O(4)(np)-COOH does not affect the diffusion limiting currents was obtained using negatively and positively charged redox active species in buffered aqueous media (pH = 7) devoid of Cd(2+). This finding made it possible to determine the concentration of unbound Cd(2+) in solutions containing dispersed Fe(3)O(4)(np)-COOH, 8 and 17 nm in diameter, directly from the Levich equation. The results obtained yielded Cd(2+) adsorption efficiencies of ~20 μg of Cd/mg of Fe(3)O(4)(np)-COOH, which are among the highest reported in the literature employing ex situ methods. Desorption of Cd(2+) from Fe(3)O(4)(np)-COOH, as monitored by the same forced convection method, could be accomplished by lowering the pH, a process found to be highly reversible.     

Porous Teflon ring-solid disk electrode arrangement for differential mass spectrometry measurements in the presence of convective flow generated by a jet impinging electrode in the wall-jet configuration

A porous Teflon ring|solid disk electrode is herein described specifically designed for acquiring online mass spectrometric measurements under well-defined forced convection created by liquid emerging from a circular nozzle impinging on the disk under wall-jet conditions. Measurements were performed for the oxidation of hydrazine, N(2)H(4), in a deaerated phosphate buffer electrolyte (pH 7) on Au, a process known to yield dinitrogen as the product. The N(2)(+) ion currents, measured by the mass spectrometer, i(N(2)(+)), as well as the corresponding polarization curves recorded simultaneously displayed very similar s-like shapes when plotted as a function of the potential applied to the Au disk. In fact, the limiting currents observed both electrochemically and spectrometrically were found to be proportional to [N(2)H(4)]. However, the limiting values of i(N(2)(+)) did not increase monotonically with the flow rate, ν(f), reaching instead a maximum and then decreasing to values independent of ν(f). This behavior has been attributed in part to hindrances in the mass transport of gases through the porous materials.     

Advancing direct ethanol fuel cell operation at intermediate temperature by combining Nafion-hybrid electrolyte and well-alloyed PtSn/C electrocatalyst

The advancement of direct ethanol fuel cell (DEFC) represents a real challenge to electrochemical science because ethanol changes significantly the triple phase boundary properties such as the redox reactions and the proton transport. Ethanol molecules promote poor fuel cell performance due to their slow oxidation rate, reduction of the proton transport due to high affinity of ethanol by the membrane, and due to mixed potential when the ethanol molecules reach the cathode by crossover. DEFC performance has been improved by advances in the membranes, e.g., low ethanol crossover polymer composites, or electrode materials, e.g., binary/ternary catalysts. Herein, high temperature (130 °C) DEFC tests were systematically investigated by using optimized electrode and electrolyte materials: Nafion-SiO₂ hybrid electrolyte and well-alloyed PtSn/C electrocatalyst. By optimizing both the electrode and the electrolyte in conjunction, DEFCs operating at 130 °C exhibited a threefold increase on performance as compared to standard commercially available materials.