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.     

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.