Structure−Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents

Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub-tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogues and their structure-activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure-dependent manner. Detailed analysis revealed a key role of the substitution pattern on the aromatic ring and a marked effect of the side chain on the activity against these two parasites. The high antileishmanial potency and remarkable selectivity of the nitro-aromatic derivatives suggested them as promising candidates for further studies. On the other hand, the high in vitro potency of catechol-type compounds against T. brucei could not be extrapolated to an in vivo mouse model.     

FDTD simulation of 30 /spl mu/m diameter polymer micro-ring

Numerical results on polymer surrounded by an air micro-ring coupled to waveguides are presented. The FDTD method predicts a filter width of 1.4 nm and an extraction efficiency of almost 80% for a gap of 0.15 /spl mu/m.     

Incorporation of Very Insoluble Monomers in Waterborne Coatings

The benefits of polymerizing very insoluble monomers in aqueous media, avoiding the use of energy‐intensive procedures, by implementing two novel synthesis techniques based on the emulsifier combination in emulsion polymerization and on miniemulsification by phase inversion temperature are investigated. The performance of standalone polymers consisting of monomers, namely lauryl methacrylate, isobornyl acrylate, and 1H,1H,2H,2H‐perfluorodecyl acrylate, and of formulated binders with these monomers incorporated either through blending or in situ polymerization, is evaluated with special emphasis on their water‐barrier properties (e.g., uptake, whitening, immersion, and vapor resistance) and on their chemical resistance. The performance of the standalone polymers is found to be similar to that of polymers prepared by high‐shear miniemulsion polymerization, while the performance of the formulated binders is generally superior to a commercial coating formulation based on a binder recommended for water resistance.     

MnO2-Based Electrochemical Supercapacitors on Flexible Carbon Substrates

Manganese dioxide films were grown on large area flexible carbon aerogel substrates. Characterization by x-ray diffraction confirmed α-MnO₂ growth. Three types of films were compared as a function of hexamethylenetetramine (HMTA) concentration during growth. The highest concentration of HM TA produced MnO₂ flower-like films, as observed by scanning electron microscopy, whose thickness and surface coverage lead to both a higher specific capacitance and higher series resistance. Specific capacitance was measured to be 64 F/g using a galvanostatic setup, compared to the 47 F/g-specific capacitance of the carbon aerogel substrate. Such supercapacitor devices can be fabricated on large area sheets of carbon aerogel to achieve high total capacitance.     

Multilayer Stacked Low‐Temperature‐Reduced Graphene Oxide Films: Preparation,Characterization, and Application in Polymer Memory Devices

Highly reduced graphene oxide (rGO) films are fabricated by combining reduction with smeared hydrazine at low temperature (e.g., 100 °C) and the multilayer stacking technique. The prepared rGO film, which has a lower sheet resistance (≈160–500 Ω sq⁻¹) and higher conductivity (26 S cm⁻¹) as compared to other rGO films obtained by commonly used chemical reduction methods, is fully characterized. The effective reduction can be attributed to the large “effective reduction depth” in the GO films (1.46 µm) and the high C1s/O1s ratio (8.04). By using the above approach, rGO films with a tunable thickness and sheet resistance are achieved. The obtained rGO films are used as electrodes in polymer memory devices, in a configuration of rGO/poly(3‐hexylthiophene) (P3HT):phenyl‐C61‐butyric acid methyl ester (PCBM)/Al, which exhibit an excellent write‐once‐read‐many‐times effect and a high ON/OFF current ratio of 10⁶.     

Absolute quantification of perfusion using dynamic susceptibility contrast MRI: pitfalls and possibilities

Absolute quantification of cerebral blood flow, cerebral blood volume and mean transit time is desirable in the determination of tissue viability thresholds and tissue at risk in acute ischaemic stroke, as well as in cases where a global reduction in cerebral blood flow is expected, for example, in patients with dementia or depressive disorders. Absolute values are also useful when comparing sequential examinations of tissue perfusion parameters, for example, in the monitoring and follow-up of various kinds of therapy. Regardless of the method employed, a number of assumptions and approximations must be made to obtain absolute measures of perfusion. Furthermore, the different stages of data acquisition and processing are associated with various degrees of uncertainty. In this review, the problems of particular relevance to absolute quantification of cerebral perfusion parameters using dynamic susceptibility contrast magnetic resonance imaging are discussed, and possible solutions are outlined.     

Rapid Up-regulation of IkappaBbeta and abrogation of NF-kappaB activity in peritoneal macrophages stimulated with lipopolysaccharide

Lipopolysaccharide (LPS) administration to mice elicited the activation of nuclear factor kappaB (NF-kappaB) in several tissues including liver and macrophages. Maximal activation was observed 1 h after treatment but declined at 3 and 6 h. The levels of IkappaBalpha and IkappaBbeta were analyzed during this period in an attempt to correlate NF-kappaB activity with IkappaB resynthesis. Degradation of IkappaBalpha was very rapid and was followed by recovery 1 h after LPS administration. IkappaBbeta degradation, which has been associated with persistent NF-kappaB activation, was complete at 1 h. However, a rapid recovery of IkappaBbeta in these tissues was observed at 3 h in parallel with the abrogation of NF-kappaB activity. Immunolocalization of newly synthesized IkappaBbeta by confocal microscopy revealed its preferential accumulation in the cytosol. Analysis of IkappaBbeta by Western blot using high resolution polyacrylamide gel electrophoresis showed the presence of two bands in cytosolic extracts of LPS-treated macrophages at 3 h, but only one band with the same mobility as the control was detected at 6 h. Moreover, treatment of extracts of resynthesized IkappaBbeta with alkaline phosphatase resulted in the accumulation of the protein of slightly higher electrophoretic mobility, indicating the prevalence of a rapid phosphorylation of the newly synthesized IkappaBbeta. At the mRNA level, up-regulation of IkappaBbeta was observed in macrophages stimulated for 1 h with LPS. When the effect of pro-inflammatory cytokines was investigated, tumor necrosis factor alpha, but not interleukin-1 or interferon-gamma, promoted an important degradation of IkappaBbeta followed by an increase in the mRNA at 1 h. These results suggest the existence of LPS- and tumor necrosis factor alpha- specific pathways involved in a rapid IkappaBbeta degradation and resynthesis and might explain the transient period of activation of NF-kappaB in these tissues upon stimulation with these factors. This rapid control of NF-kappaB function may contribute to the attenuation of the inflammatory response of these cells.     

Determination of horizontal permeability from the elliptical flow of horizontal wells using conventional analysis

Besides the regular four flow regimes normally seen during a pressure test of horizontal wells, it is possible, under special circumstances, to observe such additional flow regimes as spherical, hemi-radial, linear (reservoir channel) and elliptical. The last flow regime is characterized by a slope of 0.36 of the pressure derivative curve and occurs between the early linear flow and the pseudo-radial flow periods. This may have been overlooked in horizontal well test analysis, because it is often masked by the other flow regimes, unless the conditions are just right.The elliptical flow regime has been previously mentioned by very few researchers, Issaka et al. [Issaka, M.B., Zaoral, K., Ambastha, A.K. and Mattar, L., 2000: “Determination of Horizontal Permeability Anisotropy from Horizontal Well Tests,” SPE Saudi Arabia Section Technical Symposium, Dhahran, Saudi Arabia, 21–23 October.], Chacon et al. [Chacon, A., Djebrouni, A. and Tiab, D., 2004. “Determining the Average Reservoir Pressure from Vertical and Horizontal Well Test Analysis Using Tiab's Direct Synthesis Technique”. SPE 88619, Proceedings, SPE Asia Pacific Oil & Gas Conf. & Exhibition, Perth, Australia, 18–20 October.] and Escobar et al. [Escobar, F.H., Munoz, O.F., and Sepulveda, J.A., 2004. “Horizontal Permeability Determination from the Elliptical Flow Regime for Horizontal Wells”. CT&F — Ciencia, Tecnología y Futuro. Vol. 2 Num. 5. p. 83–95. Dec.]. A methodology for its characterization has been also introduced using the pressure derivative concept and TDS technique [Escobar, F.H., Munoz, O.F., and Sepulveda, J.A., 2004. “Horizontal Permeability Determination from the Elliptical Flow Regime for Horizontal Wells”. CT&F — Ciencia, Tecnología y Futuro. Vol. 2 Num. 5. p. 83–95. Dec.]. However, conventional analysis for the characterization of this has not yet been reported in the literature. This flow regime is very useful to estimate the horizontal permeability, especially, when the pseudo-radial flow is very short or unclear, or simply, when it is desired to verify that estimation.In this paper, equations for the estimation of the horizontal permeability and elliptical skin factor are developed for both gas and oil horizontal wells, so that the mentioned parameters can be estimated, respectively, from the slope and intercept of linear plot of pressure versus time to the power 0.36. The equations were successfully tested with two field examples previously worked in the literature.