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.     

Experimental and numerical analysis of the influence of cable tray arrangements on the resulting mass loss rate and fire spreading

In the context of industrial buildings and power plants, electrical installations and cable trays represent a main fuel load and a potential initial fire source due to possible short circuits or comparable malfunction. Furthermore, a fire can spread from one tray to additional trays mounted above and/or horizontally on one tray. Because of the high significance of cable fires, several research projects have been carried out, investigating the fire behaviour of cables from small‐scale tests, eg, the cone calorimeter, up to large‐scale tests, analysing complete cable tray constructions. The goal of the work presented in this paper is the extension of the knowledge regarding the influence of geometrical parameters like the packing density and tray distance on the burning behaviour and fire spread of cable tray installations. The results are considered, together with test results from the literature, to quantify the main physical parameters describing the burning behaviour. In a next step, the general applicability of these parameters as input data for the parametrization of the source term of numerical simulations is shown. The test results show that the burning behaviour and the fire spreading highly depend on the cable arrangement of the cables on the cable tray, in combination with other boundary conditions. By applying the results as input for a fire simulation, the mass loss rate is considered appropriately.     

Dielectric relaxation of vegetable-based polyurethane

Vegetable-based polyurethane (PU) was prepared in the thin film form by spin coating. This polymer is synthesised from castor oil, which can be extracted from the seeds of a native plant in Brazil called mamona. This polymer is biocompatible and is being used as material for artificial bone. The PU was characterised by dielectric spectroscopy in a wide range of frequency (10^–5 Hz to 10⁵ Hz) and by thermally stimulated discharge current (TSDC) measurements. The glass transition temperature (T _g = 39°C) was determined and using the initial rise method the activation energy was found to be 1.58 eV.     

Training and optimization of an artificial neural network controlling a hybrid power filter

A hybrid power compensator (HPC) consisting of a static VAr compensator and a dynamic compensator needs to be optimally controlled during the compensation of nonlinear loads. The HPC must be controlled to meet minimum requirements in terms of power factor and harmonic distortion, while at the same time minimizing its total cost. An artificial neural network (ANN) is used to control the HPC amidst a very dynamic power system environment. The performance of a reference ANN is evaluated while controlling an HPC connected to a typical nonlinear industrial load. The training and performance of the ANN is then optimized in terms of training set size, training set packing and ANN topology and the performance compared to the reference ANN. This paper highlights the importance of optimising the mentioned ANN parameters to achieve optimum ANN training and modeling accuracy. The results obtained reveals that the application of an ANN in controlling an HPC is feasible given that the ANN parameters are chosen appropriately.     

Changes in Volatile Components of Stored Tangerines and Other Specialty Citrus Fruits with Different Coatings

ABSTRACT: Shellac and wax-based citrus coatings were applied to Fallglo, Robinson, Sunburst, Dancy and Murcott tangerines, Nova and Orlando tangelos, and Temple oranges. Flavor volatiles were measured before and after storage. Concentrations of ethyl acetate, ethyl butyrate, isopentanol and 2-methyl-3-buten-2-ol increased markedly for fruit with shellac-based coatings, and were highly correlated with ethanol content, but at different ratios for the different varieties. The concentration increases were relatively less for fruit coated with the wax-based coatings, and suggest that high-gloss shellac and resin-based coatings are not appropriate for tangerines.     

台北101层国际金融中心之结构施工技术与其设计考量概述

本文旨在简要说明目前正在施工中之超高层大楼—台北国际金融中心之结构系统、钢结构工程、钢筋混凝土工程基础与深开挖工程等特殊施工技术,并佐以相关之设计考量与施工规划概要,以供工程界做参考。     

Clarification of a wheat straw‐derived medium with ion‐exchange resins for xylitol crystallization

BACKGROUND: Xylitol bioproduction from lignocellulosic residues comprises hydrolysis of the hemicellulose, detoxification of the hydrolysate, bioconversion of the xylose, and recovery of xylitol from the fermented hydrolysate. There are relatively few reports on xylitol recovery from fermented media. In the present study, ion‐exchange resins were used to clarify a fermented wheat straw hemicellulosic hydrolysate, which was then vacuum‐concentrated and submitted to cooling in the presence of ethanol for xylitol crystallization. RESULTS: Sequential adsorption into two anion‐exchange resins (A‐860S and A‐500PS) promoted considerable reductions in the content of soluble by‐products (up to 97.5%) and in medium coloration (99.5%). Vacuum concentration led to a dark‐colored viscous solution that inhibited xylitol crystallization. This inhibition could be overcome by mixing the concentrated medium with a commercial xylitol solution. Such a strategy led to xylitol crystals with up to 95.9% purity. The crystallization yield (43.5%) was close to that observed when using commercial xylitol solution (51.4%). CONCLUSION: The experimental data demonstrate the feasibility of using ion‐exchange resins followed by cooling in the presence of ethanol as a strategy to promote the fast recovery and purification of xylitol from hemicellulose‐derived fermentation media. Copyright © 2008 Society of Chemical Industry     

The function of bleaching earths in the processing of palm,palm kernel and coconut oils

The results presented in the literature, which attempt to elucidate the mechanisms by which triglyceride oils are bleached by earths, are reviewed. The impact of this work and how the mechanistic proposals affect changes in oil properties are considered, with particular emphasis on the needs of the palm oil processor. Important properties include color, metals and phosphorus content and oxidative stability of the oil. Investigations made in our own laboratories have been aimed at elucidating the effect of varying physical and chemical properties of the bleaching earth on the quality of bleached and deodorized oils. Techniques used in this work are pore-size distribution, surface area, scanning and transmission electron microscopy and a variety of chemical and X-ray analysis methods. The ability to vary such parameters in montmorillonite clays by alteration of process conditions to give materials with specific performance characteristics is demonstrated. Comparisons are made between acid-activated montmorillonites and other clay types.     

,,Rich Internet Applications“ – Eine perfekte Kombination benutzerfreundlicher Schnittstellen mit Webtechnologie

Zusammenfassung  ,,Rich Internet Applications“ (RIA) sind Webapplikationen, die mit einer wesentlich interaktiveren Benutzerschnittstelle ausgestattet sind, als wir das bisher von den auf HTML basierten ,,poor ugly web applications“ (PUWA) gewohnt waren.