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.     

包含热模型的大功率MOSFET新型电路模型

功率转换器的功率密度越来越高，发热问题越来越严重，这种功率转换器的设计对现代大功率半导体技术提出了新的挑战；因而，热问题的优化设计和核实变得比大功率器件的电模型更加重要，本文提出一种新的PSPICE模型，可以利用它计算MOSFET芯片在瞬变过程中的温度。其中的热阻可以从制造商提供的产品使用说明书得到。本文介绍的模型提供发热和电气参数之间的动态关系。它建立了与许可的热环境的关系，例如，栅极驱动电路、负载、以及散热器的分析与优化设计。利用这个模型可以改善散热器的设计。由于决定功率损耗的参数是分布在一定范围内，受生产制造的影响很大，因而散热器的设计往往由于无法预先知道功率损耗而无法进行。     

Immobilization of an endopectinlyase on γ-alumina: Study of factors influencing the biocatalytic matrix stability

Endopectinlyase (EC 4.2.2.10) from Aspergillus japonicus was immobilized on to γ-alumina. Adsorption performed at pH 5·0 and a subsequent cross-linking phase using 0·1% glutaraldehyde were the chosen immobilization conditions. The comparison between the main biochemical parameters of the immobilized and free form of the enzyme showed that the immobilization procedure used did not affect the enzyme biochemical properties. The interactions between the carrier and the enzyme are essentially secondary bonding. In fact they depend on the pH and on the presence of phosphate ions in the medium. A tentative chemical model of the biocatalytic matrix thus obtained is proposed.     

Variable-gain up-converter with current reuse for 5-GHz WLAN applications

A variable-gain up-conversion mixer for 5-GHz WLAN applications is presented, whose input stage is based on a novel variable gain transconductor. The proposed topology features reduced power consumption by exploiting dc current reuse for mixer biasing. Moreover, a new low-consumption control circuit is introduced, which achieves a temperature-stable and linear-in-dB characteristic, providing a 40-dB dynamic range within ±1 dB gain error.     

Surface tension as a limiting factor for aerobic n-alkane biodegradation

A new mathematical model for n-alkane biodegradation in crude oil, heavy oil and paraffinic mixtures is described. The pattern of n-alkane degradation as a function of the inverse of hydrocarbon chain length reported in this paper can be considered as general behaviour for many aerobic n-alkane biodegradation processes. A new interpretation of n-alkane biodegradation as a function of surface tension, is given. A mathematical expression was obtained starting from the degradation values of n-alkane and relative surface tension, which is a parameter independent of fermentation conditions. An interesting parameter, b, was identified which represented the accelerating conversion factor for n-alkane biodegradation. The findings suggested that the n-alkane biodegradation. The findings suggested that he n-alkane biodegradation rate may be affected by the fermentation condition (agitation, aeration, etc.) and by the strain of microorganism, while the behaviour pattern of n-alkane degradation was essentially linked to the substrate characteristics (molecular structure, molecular weight and density).     

Macrophage-derived cytokines in the follicular fluids of women with infertility due to immunological causes. Elevated levels of interleukin 6 and low levels of granulocyte-macrophage colony-stimulating factor

Myoclonus of the middle ear is a rare condition characterized by abnormal repetitive muscle contractions of the tympanic cavity. In this paper we describe what we believe is the first reported case of continuous high-frequency objective tinnitus caused by middle ear myoclonus. During exploratory tympanomastoidectomy it was hypothesized that a small dural arteriovenous malformation not identified on previous tests was the cause of the tinnitus. However, complete disappearance of the tinnitus during administration of curare for anesthesia led us to believe that the tinnitus might have been caused by myoclonus of the middle ear. Sectioning of the stapedius and tensor tympani tendons rendered the patient asymptomatic and confirmed the diagnosis of middle ear myoclonus. At follow-up of one year, the patient's quality of life had improved substantially; the tinnitus did not recur and she no longer had vertigo.     

Manufacturing of polypropylene laminates and related structural reorganization in the crystalline phase

The conditions for obtaining recrystallization in more ordered modifications are described for an uniaxially oriented sample of isotactic polypropylene, annealed with fixed ends. These recrystallization conditions are related to the conditions of a lamination process.     

Proteomic profile of differentially expressed plasma proteins from dystrophic mice and following suberoylanilide hydroxamic acid treatment

Purpose: Histone Deacetylase Inhibitors (DI) ameliorates dystrophic muscle regeneration restoring muscular strength in the mdx mouse model of Duchenne muscular dystrophy (DMD). The further development of these compounds as drugs for DMD treatment is currently hampered by the lack of knowledge about DIs effect in large dystrophic animal models and that of suitable biomarkers to monitor their efficacy. Experimental design: In this study we applied proteomic analysis to identify differentially expressed proteins present in plasma samples from mdx mice treated with the Suberoylanilide hydroxamic acid (SAHA) and relative normal controls (WT). Results: Several differentially expressed proteins were identified between untreated wild type and mdx mice. Among these, fibrinogen, epidermal growth factor 2 receptor, major urinary protein and glutathione peroxidase 3 (GPX3) were constitutively up‐regulated in mdx, while complement C3, complement C6, gelsolin, leukaemia inhibitory factor receptor (LIFr), and alpha 2 macroglobulin were down‐regulated compared to WT mice. SAHA determined the normalization of LIFr and GPX3 protein level while apoliprotein E was de novo up‐regulated in comparison to vehicle‐treated mdx mice. Conclusions and clinical relevance: Collectively, these data unravel potential serological disease biomarkers of mdx that could be useful to monitor muscular dystrophy response to DI treatment.     

Ultimate behavior of axially loaded RC wall-like columns confined with GFRP

The assessment of the effectiveness of the fiber reinforced polymer (FRP) confinement on rectangular reinforced concrete (RC) columns with high aspect ratio (wall-like) still represents an unresolved issue. The present paper aims at providing more experimental evidence about the behavior of such members confined with both uni-directional and quadri-directional glass FRP laminates. Particular attention is devoted to issues related to the premature failure of confining fibers experimentally observed in wall-like columns. Test results on nine axially loaded columns are herein presented; emphasis is also given to the analysis of FRP strain profiles along the sides of the cross-section. The analysis of test results highlights that glass FRP (GFRP) confinement could determine significant strength and ductility increases; the discussion of failure modes points out that the failure of GFRP confined wall-like columns is controlled by the shape of the cross-section and occurs at transverse strains in the jacket much lower than those ultimate of the fibers. Theoretical–experimental comparisons are performed using some available models for strength prediction of such members.