Synthesis and Biological Evaluation of Papain‐Family Cathepsin L‐Like Cysteine Protease Inhibitors Containing a 1,4‐Benzodiazepine Scaffold as Antiprotozoal Agents

Novel papain‐family cathepsin L‐like cysteine protease inhibitors endowed with antitrypanosomal and antimalarial activity were developed, through an optimization study of previously developed inhibitors. In the present work, we studied the structure–activity relationships of these derivatives, with the aim to develop new analogues with a simplified and more synthetically accessible structure and with improved antiparasitic activity. The structure of the model compounds was significantly simplified by modifying or even eliminating the side chain appended at the C3 atom of the benzodiazepine scaffold. In addition, a simple methylene spacer of appropriate length was inserted between the benzodiazepine ring and the 3‐bromoisoxazoline moiety. Several rhodesain and falcipain‐2 inhibitors displaying single‐digit micromolar or sub‐micromolar antiparasitic activity against one or both parasites were identified, with activities that were one order of magnitude more potent than the model compounds.     

Intramolecular Direct Arylation and Heck Reactions in the Formation of Medium‐Sized Rings: Selective Synthesis of Fused Indolizine,Pyrroloazepine and Pyrroloazocine Systems

The intramolecular palladium‐catalyzed reaction of N‐(iodoarylalkyl)pyrroles can be applied for the selective synthesis of medium‐sized rings by choosing the appropriate catalytic systems to direct the reaction to the alkene or to the pyrrole nucleus. These reactions can also be extended to the corresponding heteroaryl halides. Thus, reaction conditions have been established to access selectively to (hetero)fused indolizine, pyrroloazepine and pyrroloazocine systems.

     

Carbon and sulfur cycling by microbial communities in a gypsum-treated oil sands tailings pond

Oil sands tailings ponds receive and store the solid and liquid waste from bitumen extraction and are managed to promote solids densification and water recycling. The ponds are highly stratified due to increasing solids content as a function of depth but can be impacted by tailings addition and removal and by convection due to microbial gas production. We characterized the microbial communities in relation to microbial activities as a function of depth in an active tailings pond routinely treated with gypsum (CaSO(4)·2H(2)O) to accelerate densification. Pyrosequencing of 16S rDNA gene sequences indicated that the aerobic surface layer, where the highest level of sulfate (6 mM) but no sulfide was detected, had a very different community profile than the rest of the pond. Deeper anaerobic layers were dominated by syntrophs (Pelotomaculum, Syntrophus, and Smithella spp.), sulfate- and sulfur-reducing bacteria (SRB, Desulfocapsa and Desulfurivibrio spp.), acetate- and H(2)-using methanogens, and a variety of other anaerobes that have been implicated in hydrocarbon utilization or iron and sulfur cycling. The SRB were most abundant from 10 to 14 mbs, bracketing the zone where the sulfate reduction rate was highest. Similarly, the most abundant methanogens and syntrophs identified as a function of depth closely mirrored the fluctuating methanogenesis rates. Methanogenesis was inhibited in laboratory incubations by nearly 50% when sulfate was supplied at pond-level concentrations suggesting that in situ sulfate reduction can substantially minimize methane emissions. Based on our data, we hypothesize that the emission of sulfide due to SRB activity in the gypsum treated pond is also limited due to its high solubility and oxidation in surface waters.     

Energy transfer and compatibility analysis of PVK/MEH-PPV blends processed via electrospraying and electrospinning

Solution polymer blends of a high molecular weight and a low molecular weight poly(9-vinyl carbazole) PVK with poly[2-methoxy-5-(2′-ethylhexyloxy)-1,4-phenylenevinylene] (MEH-PPV), at a fixed blend ratio of 95.5:0.5, were processed via electrospraying and electrospinning. SEM studies revealed that electrosprayed particles were produced when low molecular weight PVK was used, while electrospun fibers were successfully obtained from solutions containing high molecular weight PVK, over a concentration range of 4–10% (w/v). From the absorption spectra of the neat polymers it was determined that Urbach energy E_u increase and optical band gap E_g decreases due to the physical defects along the main chain introduced by these electrostatic processing methods. Photoluminescence spectroscopy revealed a particular applied voltage, which depends on concentration and molecular weight, where aggregation of PVK levels off. Luminescence quenching of MEH-PPV is also observed to increase with applied voltage consistent with possible energy transfer from shorter conjugation length segments to nearby longer conjugated segments. The ratio of the intensity of the excitation spectra of the PVK (donor, both PVK_L or PVK_H) and the MEH-PPV (acceptor), I_D/I_A, exhibited minima at this particular voltage and then levels off, indicating not only maximum interpenetration and thus compatibility of both polymers but also maximum energy transfer. Hence, we demonstrate that compatibility and energy transfer can be optimized varying concentration and applied voltage during both electrospraying and electrospinning processes.     

High performance liquid chromatographic detection of a strongly retained pigment fraction in Capsicum annuum

A new colour pigment fraction was detected in Capsicum annuum by high performance liquid chromatography. Surprisingly the pigment was strongly bound both to silica and octadecylsilica surfaces indicating that its molecular mass is probably high. Peak purity tests proved that the fraction is not homogeneous and the degree of inhomogeneity depends on the wavelength used for the peak purity test. The spectra taken at one minute intervals of the peak were strikingly different supporting the above conclusions. It is possible that this highly lipophilic pigment is a secondary product of the ripening and processing procedures and is a mixture of individual pigments covalently bound to each other.     

Al surface morphology effect on flip-chip solder bump shear strength

This paper reports the result of a study on the effect of aluminum pad surface morphology on the flip-chip solder bump reliability. The influence of the Al surface morphology on the electroless zinc/nickel/gold UBM is presented. The reliability of the solder bump as measured by ball shear force is reported. Al pad were produced using two RF sputtering systems: CVC-601 and Varian-3180. The Al targets used in CVC and Varian system were 99%Al–1%Si and 98.95%Al–1%Si–0.05%Ti respectively. The surface of the CVC sputtered Al samples were smooth while the surface of the Varian sputtered Al samples were rough. All the samples were subjected to the electroless zinc/nickel/gold plating. The results suggest that after plating, the smooth Al surface resulted in a fine nickel UBM surface while the rough Al surface formed a coarse nickel UBM surface. Ball shear test was conducted after the solder balls were bumped on the UBM. Result shows that the fine UBM surface samples have twice the shear strength compared to the samples with coarse UBM surface samples. The analysis of the results indicates that shear surface occurred at the UBM and the solder interface for samples with rough UBM surface leading to the lower shear strength. Nickel bump shear test result shows that pretreatment of Al pad surface by sodium hydroxide and nitric acid created more zinc seeds this led to better electroless nickel plating. Nickel bump shear tests also shows that double zincated bumps had higher shear strength than single zincated bumps. To obtain reliable flip-chip solder bumps, it is essential to maintain good Al pad surface morphology, pretreatment of the Al pad and undergo second zincation.     

Behavioral science activities at the Centers for Disease Control and Prevention: A selected overview of exemplary programs.

Behavioral research and surveillance activities are conducted across the Centers for Disease Control and Prevention (CDC). This article highlights activities in 4 program areas: violence against women, tuberculosis elimination, HIV prevention, and occupational health. The unique constraints and opportunities of each organization and program focus have shaped the way research has developed in each of these areas. Behavioral scientists also face many common challenges at CDC. Despite the difficulties of integrating behavioral research into an institution that historically has focused on biomedical and epidemiological research, behavioral scientists have made important contributions to public health. Many opportunities remain for psychologists to translate theory and operationalize constructs for use in solving important public health problems. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

STUDY OF GLAZE PENETRATION AND ITS EFFECT ON GLAZE FIT: I-III*

A method for determining glaze penetration was developed and the effect of glaze penetration on glaze fit studied. The effects of twenty-four fluxes on penetration of a base glaze into semivitreous, hotel china, terra cotta, cordierite, pyrophyllite, wall tile, and steatite bodies were determined. The result shows that glaze penetration affects glaze fit and that penetration varies greatly, depending on glaze composition and the character of the body.     

Effects of outliers on the identification and estimation of GARCH models

Abstract. This paper analyses how outliers affect the identification of conditional heteroscedasticity and the estimation of generalized autoregressive conditionally heteroscedastic (GARCH) models. First, we derive the asymptotic biases of the sample autocorrelations of squared observations generated by stationary processes and show that the properties of some conditional homoscedasticity tests can be distorted. Second, we obtain the asymptotic and finite sample biases of the ordinary least squares (OLS) estimator of ARCH(p) models. The finite sample results are extended to generalized least squares (GLS), maximum likelihood (ML) and quasi‐maximum likelihood (QML) estimators of ARCH(p) and GARCH(1,1) models. Finally, we show that the estimated asymptotic standard deviations are biased estimates of the sample standard deviations.     

Note on a simple algorithm for a computer-produced reading ease score.

Describes 3 relatively simple computer algorithms for estimating the average number of syllables/word in text from letter counts. The syllable counts were used to determine Flesch Reading Ease Scores for text by computer. Vowel counts worked well. (PsycINFO Database Record (c) 2010 APA, all rights reserved)