Synthesis of a small library of non-symmetric cyclic sulfamide HIV-1 protease inhibitors

A set of 11 non-symmetric cyclic sulfamide HIV-1 protease inhibitors were synthesized and evaluated. The use of a key microwave-assisted silver(I) oxide mediated selective mono N-benzylation reaction enabled fast and straightforward synthesis. The K_i values of the new inhibitors ranged between 0.28 μM and >20 μM.     

Slow dynamics of a colloidal lamellar phase

We used x-ray photon correlation spectroscopy to study the dynamics in the lamellar phase of a platelet suspension as a function of the particle concentration. We measured the collective diffusion coefficient along the director of the phase, over length scales down to the interparticle distance, and quantified the hydrodynamic interaction between the particles. This interaction sets in with increasing concentration and can be described qualitatively by a simplified model. No change in the microscopic structure or dynamics is observed at the transition between the fluid and the gel-like lamellar phases.     

The Re(I) coordination chemistry of a series of pyrido[2,3-b]pyrazine-derived ligands: Syntheses,characterisation and crystal structures

Reaction of 2,3-diaminopyridine with one equivalent of a functionalised vicinal diketone, in ethanol, yields a series of ligands based upon the pyrido[2,3-b]pyrazine core. The ligands were characterised by ¹H, ¹³C–{¹H} NMR, MS and UV–Vis spectroscopy. Reaction of the ligands with one equivalent of {ReBr(CO)₅} gave a series of Re-Lⁿ complexes based upon the general formula fac-{ReBr(CO)₃(L)} (where L = pyrido[2,3-b]pyrazine-derived ligands, L¹–L⁶). Solution IR studies confirmed the retention of the facially capped, tri-carbonyl coordination geometry at rhenium, and ¹H NMR studies confirmed coordination of the ligand to Re(I). EI HR MS data were obtained for each complex confirming the proposed formulation and stoichiometry. Single crystal X-ray structures were obtained for three of the complexes (Re-L¹, Re-L², Re-L⁶), with each demonstrating that the ligands coordinate to Re(I) in a bidentate manner, via a four-membered chelate ring, which was unsymmetrical in the former two cases. The electronic absorption spectra of the complexes showed absorption into the visible region ca. 375–500 nm, (the complexes are orange-red in appearance). Following irradiation at 350–450 nm, the complexes display a solid-state broad emission peaking between 600–700 nm. The complexes were not sufficiently luminescent in solution to allow further investigation into the origin of this emission band, although with reference to related 1,8-naphthyridine complexes of Re(I) it is likely to incorporate significant ³MLCT character.     

Accelerated 18O-labeling in urinary proteomics

Proteolytic (18)O-labeling of peptides has been studied and optimized in order to improve the labeling efficiency and to accelerate the process without increasing the degree of incomplete labeling. Using peptides generated from tryptic digested bovine serum albumin (BSA) and cytochrome c as model proteins, it was shown that complete labeling was achieved after 2 h at pH 6. To increase the sample throughput in a bottom-up proteomic setup, tryptic digestion of proteins in-solution was replaced with tryptic digestion using immobilized trypsin. As a result, an integrated approach was made possible, where both digestion (pH 8) and (18)O/(16)O-labeling of the resulting peptides (pH 6) were done using immobilized trypsin beads. This simplified the sample handling and reduced the overall reaction time significantly: the setup enabled tryptic digestion and (18)O/(16)O-labeling without sample transfer steps within 3.5 h with average (18)O/(16)O-ratios of 0.96±0.13 in aqueous buffer. The initial results were confirmed with a more complex matrix, by spiking urine with the model proteins, yielding results comparable with the ratios obtained in buffer. Satisfying ratios were also achieved regarding urinary proteins identified in a full scale bottom-up experiment. Average (18)O/(16)O-peptide ratios of 0.83±0.13 and 0.91±0.27 indicated good performance in a highly relevant matrix for biomarker discovery.     

Vowel-related tongue movements in speech: straight or curved paths? (L)

This paper examines tongue movements between the two vowels in sequences of vowel-labial consonant-vowel, addressing the question whether the movement is a straight line or a curved path. Native speakers of Japanese and Italian served as subjects. The linguistic material consisted of words where the bilabial consonant was either long or short. The inclusion of words with different consonant lengths was motivated by earlier findings that the tongue movement is often longer when the consonant is long, which may be due to a more curved movement path. Tongue movements were recorded using a three-transmitter magnetometer system. To assess the movement path, the movement magnitude was calculated in two ways, as a straight line, the Euclidean distance, and as the actual path, obtained by summing the individual Euclidean distances between successive samples from movement onset to offset. The ratio between the path and the Euclidean distance is 1 when the movement is a straight line and greater than 1 when the path is curved. Results show that in virtually all 21 cases examined the ratio was very close to 1 and in most cases 1.2 or less. There was no reliable influence of consonant length on the ratio.     

Potential solutions to improved sound performance of volume based lightweight multi-storey timber buildings

Lightweight building systems in general suffer from poor sound insulation, especially in the low frequency region. Since no reliable mathematical models that can predict the impact sound pressure level exists, the lightweight building design is to a high extent based upon previous experience and upon measurements. A special difficulty is related to experimental measurements since the variation among identical units must not be neglected. A modern volume based lightweight wooden building concept has here been tested by numerous well controlled measurements, in laboratory as well as in more field like conditions. The volume construction technique offers new possibilities and challenges to improve sound insulation in light weight timber construction. The main purpose was to investigate how different constructional solutions in the floor, like plaster board, mineral wool, elastic glue, dividing board, floating floor etc., affect the sound insulation. Many of the tested modifications resulted in only marginally changed impact sound pressure level but parameters that substantially can improve the sound insulation were found in using elastic glue to mount the floor boards, to install extra board layers and to use floating floors.     

Shape of the ferromagnetic resonance absorption band of textured powder samples of maghemite

The shape of the ferromagnetic resonance absorption band of powder microcrystalline ferrite γ-Fe₂O₃ has been studied. Samples in the form of a ferromagnetic fluid have been subjected to preliminary particle orientation and frozen in a magnetic field. The shape of the absorption bands has been computer processed with allowance for the anisotropy of the shape of particles and their spatial cubic anisotropy, as well as for the contribution from nondispersed fraction of the bulk of the powder. Satisfactory agreement with the experiment has been obtained for several orientations of the measuring magnetic field with respect to the preliminary orientation.     

A fully integrated IQ-receiver for NMR microscopy

We present a fully integrated CMOS receiver for micro-magnetic resonance imaging together with a custom-made micro-gradient system. The receiver is designed for an operating frequency of 300 MHz. The chip consists of an on-chip detection coil and tuning capacitor as well as a low-noise amplifier and a quadrature downconversion mixer with corresponding low-frequency amplification stages. The design is realized in a 0.13 μm CMOS technology, it occupies a chip area of 950 × 800 μm2 and it draws 50 mA from a supply voltage of 1.8 V. The achieved time-domain spin sensitivity is 5×10(14)spins/Hz. Images of phantoms obtained in our custom-made gradient system with 8 μm isotropic resolution are reported.     

Locating replenishment stations for electric vehicles: application to Danish traffic data

Environment-friendly electric vehicles have gained popularity and increased attention in recent years. The deployment of a network of recharging stations is essential given their limited travel range. This paper considers the problem of locating electronic replenishment stations for electric vehicles on a traffic network with flow-based demand. The objective is to optimize the network performance, for example to maximize the flow covered by a prefixed number of stations or to minimize the number of stations needed to cover traffic flows. Two integer linear programming formulations are proposed to model the problem. These models are tested on real-life traffic data collected in Denmark.     

A metacognitive-based instruction for Primary Four students to approach non-routine mathematical word problems

Many Primary Four students (fourth graders) in Singapore have difficulties initiating or persevering in the problem-solving process even though the curriculum has focused on problem solving since 1992. This study served to examine the role of metacognition in self-regulated problem solving. The study, a quasi-experimental pretest–posttest design involving a convenience sample of 63 students from two intact mixed-ability Primary Four classes, examined the impact of using a metacognitive scheme that focuses on the understanding and planning stages of Pòlya’s four-stage approach on students’ mathematical problem-solving behavior, performance and attitudes. The findings revealed that the metacognitive-based scheme had a positive impact on students’ understanding of the problem posed, solution planning, confidence in and personal control of problem-solving behavior and emotions. It had also helped them to initiate and persevere in the problem-solving process to achieve a higher level of problem-solving success. Limitations and instructional implications are discussed.