New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent

A series of 5-keto-substituted 7-tert-buty1-2,3-dihydro-3,3- dimethylbenzofurans (DHDMBFs) were prepared and evaluated as potential nonsteroidal antiinflammatory and analgesic agents. Interest in this class of compounds arose when a DHDMBF was found to be an active metabolite of the di-tert-butylphenol antiinflammatory agent tebufelone. We have now found that a variety of 5-keto-substituted DHDMBFs have good in vivo antiinflammatory and analgesic activity after oral administration. These compounds inhibit both cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) in vitro. The cyclooxygenase inhibition was found to be selective for the cyclooxygenase-2 isoform, and this combination of COX-2/5-LOX inhibition may be responsible for the gastrointestinal safety of compounds such as 30.     

Transmission of mechanical energy through polymeric liquid crystals and their blends

Molecular composites, also called polymeric liquid crystals (PLC), are contrasted with the traditional composites; the name heterogeneous composites is proposed for the latter. Advantages of blending PLCs with ordinary engineering polymers are discussed. Results reported for blends of poly(ethylene terepthalate) (PET) with a PLC containing sequences of PET and p-hydroxybenzoic acid (PHB) include thermophysical properties, melt rheology, mechanical properties of solid blends, and scanning electron microscopy of fracture surfaces. A model called the island model was developed to explain the results: One assumes that the lines of force as well as propagating cracks tend to concentrate in the phase rich in the more flexible engineering polymer, avoiding the islands rich in the liquid-crystalline phase. This prevails until the phase inversion occurs. Predictions from the model are fully confirmed by the experimental evidence.     

Superconductivity Within the Pair-Tunneling Model Close to the Metal-Insulator Transition

We have considered the problem of s-wave and d-wave superconductivity in the two-layer Hubbard model close to the metal-insulator transition. To mimic the formation of the insulating gap, the Coulomb correlations have been taken into account within the Hubbard I approximation. The interlayer momentum-conserving Josephson tunneling between the layers has been included on the mean-field level. We demonstrate that the interlayer tunneling may contribute to the occurrence of mixed d + s wave symmetry of the superconducting state with a dominating d-wave component at a low concentration of holes. The problem of the validity of the pair-tunneling model is also briefly discussed.     

Molecular models of polymer networks and constitutive equations of rubber elasticity

Equilibrium elastic behaviour of crosslinked polymers (networks) is analysed both from the macroscopic (phenomenological) and microscopic (molecular) points of view. Molecular mechanisms possibly responsible for non-linear rubber elasticity are discussed. They include: conformational entropy of network chains at small and large extensions, hindered rotation of such chains and intra-chain point interactions, dipole-dipole interactions between asymmetric chain segments, and topological constraints leading to chain entanglement.     

Polymeric membranes for lipase immobilization

Lipase triacylglycerol acylhydrolase, (E.C. 3.1.1.3) is an enzyme that is fully active on aggregated substrates and practically inactive on monodisperse systems. A lipase immobilized on polymeric membranes has been applied for sunflower oil hydrolysis. The influence of membrane properties on enzyme activity is studied. Membranes made of poly(vinyl chloride), collagen, cellulose acetate and polytetrafluoroethylene were used for adsorption of lipase. The porosity and hydrophobicity of membranes did not influence the lipase activity. The difference of the work of adhesion for the water/membrane system and oil/membrane system reflected the activity data, while work of adhesion for water or oil (done separately) did not. For oil hydrolysis to occur on the membrane surface, accessibility of two liquid phases is important, and the lower the difference of work of adhesion between water and oil, the greater the activity of immobilized lipase.     

Defect Equilibria and Transport in YBa2Cu3O7-x at Elevated Temperatures: I, Thermopower, Electrical Conductivity, and Galvanic Cell Studies

Studies of the Y-Ba-Cu-O system at elevated temperatures (300 to 1173 K) and under controlled oxygen activity (10² to 10⁵ Pa) were performed by using electrical methods such as thermopower, electrical methods such as thermopower, electrical conductivity, and emf of solid-state galvanic cell measurements. The discontinuities of measured electrical parameters demarcate regions of different properties and phenomena: (a) the transition between the range when the oxide sample is quenched on one side and the equilibrium range on the other side and (b) the transition between the quasi-metallic and semiconducting (m/s) regimes. The temperature of the m/s transition increases from 950 K at p o₂= 10² Pa to 1150 K at 10⁴ Pa. These data have served to derive a T-p o₂ diagram for YBa₂Cu₃O_7-x. NO discontinuity of the measured electrical parameters has been observed under conditions accompanying the phase transition between the tetragonal and orthorhombic structures. A p-n type transition has been observed within the semiconducting regime. Electrochemical oxygen titration has led to the determination of the relationship between the lattice oxygen content and the oxygen activity in the ambient gas atmosphere.     

Photolithography illumination needs

Industrial photolithographic exposures are now performed almost entirely with the high pressure mercury arc, using one or more of the spectral lines at 365, 408 and 436 nm. It would be difficult for the free electron laser to replace the entrenched and reliable arc unless it could offer a significant improvement, for instance, in brightness. Lithography is currently being extended to shorter wavelengths, as far as the X-ray regime. At present, the excimer laser is the principal source in the UV. Since the excimer is comparatively new, the FEL might find a niche more easily in this domain. To compete with current sources in the near and far UV, the FEL should provide at least 4 W of useable power. Since lithographic illumination must be uniform, the coherence of the FEL output must be sufficiently low to avoid “noise” due to interference. In addition, a light source for industrial use must be reliable and maintainable by plant personnel.     

The effect of heating conditions on losses and regeneration of betacyanins

Summary The losses of Betacyanins during heating at 90 °C and their regeneration after heating were investigated in red beet juice and solutions of pure betanin in different buffers. It was found that the regeneration of pigments during storage of heated samples is greater at 5 °C than at 20 °C. The time, in which the pigments reach the maximum concentration is different for juice and pure betanin solutions. The influence of the type of buffer and its concentration on heating in the absence of oxygen is insignificant, on the other hand the influence is distinctly marked when the betanin heated in the presence of oxygen. When heated in the presence of air, the betanin losses are influenced by the rate of diffusion of oxygen from the air.

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Einflu der Erhitzungsbedingungen auf Verluste und Regeneration der Betacyanine

Zusammenfassung Die Verluste an Betacyaninen während der Erhitzung auf 90 °C und ihre Regeneration nach dem Erhitzen wurden in Rote-Beete-Saft und in verschieden gepufferten reinen Betanin-Lösungen untersucht. Bei 5 °C ist die Regeneration der Farbstoffe besser als bei 20 °C. Die Zeit bis zur maximalen Regeneration der Farbstoffe ist für den Saft und für die Betanin-Lösungen unterschiedlich. Pufferart und -konzentration sind unter sauerstofffreien Bedingungen unwesentlich; bei Anwesenheit von Sauerstoff üben sie indessen einen merklichen Einflu aus. Beim Erhitzen in Gegenwart von Sauerstoff werden die Betanin-Verluste von der Diffusionsgeschwindigkeit des Luftsauerstoffs beeinflußt.

     

Organosilicon resin-based carbon/ceramic polygranular composites with improved oxidation resistance

We examined the thermo-mechanical properties of carbon materials modified with silicon oxycarbide (Si-O-C) and silicon carbide (Si-C). These compounds were obtained by the impregnation of carbon components with a silicon-containing polymer resin. Graphite and anthracite powders were used as carbon components, and poly[methyl(phenyl) siloxane] resin (P) was used as the ceramic precursor. Carbon/polymer compositions (C/P) were subjected to two-stage annealing, first to 1,000 °C and next to 2,000 °C in an inert atmosphere, leading to the formation of C/Si-O-C and C/Si-C composite samples, respectively. The materials were then examined under conditions of isothermal oxidation to determine their oxidation resistance and the mechanical properties before and after oxidation tests. The structure of the samples before and after oxidation was studied. C/Si-C composites, despite their high porosity, proved to have enhanced resistance to oxidation at 600 °C, although they had lower mechanical properties in comparison to C/Si-O-C samples.