N-Substituted Nipecotic Acids as (S)-SNAP-5114 Analogues with Modified Lipophilic Domains

Potential mGAT4 inhibitors derived from the lead substance (S)-SNAP-5114 have been synthesized and characterized for their inhibitory potency. Variations from the parent compound included the substitution of one of its aromatic 4-methoxy and 4-methoxyphenyl groups, respectively, with a more polar moiety, including a carboxylic acid, alcohol, nitrile, carboxamide, sulfonamide, aldehyde or ketone function, or amino acid partial structures. Furthermore, it was investigated how the substitution of more than one of the aromatic 4-methoxy groups affects the potency and selectivity of the resulting compounds. Among the synthesized test substances (S)-1-{2-[(4-formylphenyl)bis(4-methoxyphenyl)-methoxy]ethyl}piperidine-3-carboxylic acid, that features a carbaldehyde function in place of one of the aromatic 4-methoxy moieties of (S)-SNAP-5114, was found to have a pIC₅₀ value of 5.89±0.07, hence constituting a slightly more potent mGAT4 inhibitor than the parent substance while showing comparable subtype selectivity.     

Reality-based interaction affecting mental workload in virtual reality mental arithmetic training

ABSTRACT

The concept of digital game-based learning (DGBL) evolves rapidly together with technological enhancements of virtual reality (VR) and smart phones. However, the mental workload (MWL) that VR-training applications demand and motivational qualities originating from user experience (UX) should be identified in order to create effective and enjoyable training/learning challenges that fit with individual users’ capabilities. This study examined the effects of reality-based interaction (RBI) and VR on measures of student motivation and MWL, in a mental arithmetic game for secondary school pupils. In a randomised controlled trial with sixty school children, a mental arithmetic game was tested with three different interaction and two different presentation methods – VR RBI, VR head-mounted-display tapping and tablet flick-gesture. Results found a significant effect of RBI on MWL but no differences in enjoyment of training were found between VR-experience and tablet training-experience. In fact, adding the gaming-context to the mental arithmetic task created an enjoyable, motivating experience regardless of presentation or interaction-style.     

An automated system based on cryogenic probe station for integrated studies of semiconductor light-emitting structures and wafers in the range of 15 to 475 K

An automated system for integrated electrophysical and optical studies of semiconductor nanoheterostructures, which operates in a wide temperature range from 15 to 475 K, is designed. The setup is intended to measure the temperature and frequency admittance and electroluminescence spectra of light-emitting diode and laser chips formed on substrates of diameter up to 50.2 mm, and the distribution of parameters over the wafer. The setup includes the closed-cycle helium cryogenic station, LCR meter, and temperature controller. The characterization results of nanoheterostructures with InGaN/GaN multiple quantum wells, which are used for creating highly efficient white and blue light-emitting diodes, are presented.     

Isolation of antimicrobial agent from the marine algae Cystoseira hakodatensis

Cystoseira hakodatensis is an unutilised brown algae belonging to family Sargassaceae. A crude methanol extract from the algae showed inhibitory effects on the growths of Bacillus cereus and Bacillus licheniformis. To isolate the major antimicrobial agent, a sequential active‐guided isolation procedure was applied: liquid–liquid extraction, column chromatography and bio‐autography. A marked antimicrobial agent (active α) was isolated in hydrophobic fraction and was determined to phenolics without carbohydrates and proteins by phytochemical test. Regarding the antimicrobial potential, the isolated active α showed better inhibitory effects against B. cereus and B. licheniformis at 2 and 4 times of lower concentrations (62.5 and 31.3 μg mL^?1) in comparison with epigallocatechin gallate. These results showed that C. hakodatensis is a potential source of antimicrobial agent capable of preventing the growth of the two bacteria.     

Irreversible deformation and the superplasticity of a TN-1 alloy during thermal cycling through the martensitic transformations ranges under loading

The influence of the thermal cycling conditions on the thermal-cycling creep of a TN-1 alloy and the related irreversible deformations is studied. The conditions under which an anomalous increase in the irreversible deformations begins are determined. The structural mechanism of the irreversible deformations of an equiatomic alloy is shown to be analogous to the structural mechanism of metal creep at high temperatures: it predominantly has a dislocation character. It is proposed to use the effect of anomalous increase in the deformation of materials with reversible martensitic transformations for forming parts made of these materials at low temperatures.     

Basic trends in development of drilling equipment for ore mining with block caving method

The authors have determined the causes of drop in performance of induced block caving using fans of blastholes 105 mm in diameter and single blastholes 250 mm in diameter, as well as the sources of increased drilling cost and expansion of start-up time of production blocks in Abakan underground mine. Alternatives of improvement in drilling efficiency under current conditions are discussed.