Synthesis and Biological Studies of O3-Aryl Galactosides as Galectin Inhibitors

β-Galactose derivatives have recently been reported to selectively inhibit galectin-3, and a library of O3-arylated galactosides with varying substitution patterns was designed to study such inhibitions further. The O3-arylated galactosides were synthesized using diaryliodonium salts under mild and transition metal free conditions, providing the target products in moderate to good yields. An O3-trifluoroethylated galactoside was also synthesized using iodonium salt chemistry. Azido-substituted products were subsequently transformed into the corresponding triazoles. After deprotection, a selection of galactoside derivatives were evaluated for inhibitory potencies against galectins-1, 3, 4 N (N-terminal domain), 4 C (C-terminal domain), 7, 8 N, 8 C, 9 N, and 9 C and one compound with promising affinity and selectivity for both the N- and C-terminal domain of galectin-9 was discovered.     

Amplification reduction in fiber amplifiers due to up-conversion at Er3 concentrations below 1000 ppm

The parasitic effect of two-ion up-conversion in Er³⁺ -doped fibers have been investigated. Maximum amplification for eight different Er³⁺ concentrations have been measured and it is shown that up-conversion drastically reduces amplification for Er³⁺ concentrations in the range of 140-1680 ppm by weight. We have also measured an up-conversion induced luminescence at 980 nm. By comparison of experimental and simulated characteristics, we obtain an up-conversion coefficient of 10^-22 m³/s.     

2,3,5,6-Tetramethylmorpholine: II—1H n.m.r. structural studies of the isomers of 2,3,5,6-tetramethylmorpholine

The structures of the six isomers of 2,3,5,6-tetramethyl-morpholine have been determined by means of proton nuclear magnetic resonance studies at 100 MHz. The spectra have been analysed in terms of spin–spin coupling constants and population distributions of the possible conformers at low temperatures. Also included in this paper are results from n.m.r. studies on the six 4-benzyl-2,3,5,6-tetramethylmorpholine derivatives, which give information about the stereochemistry of the methyl groups α to the amine group.     

Barriers to internal rotation in 1,3,5-trineopentylbenzenes—II: Unsymmetrically halogen-substituted compounds

The temperature dependence of the three different methylene AB spectra due to the 1-, 3- and 5-neopentyl groups in 2-chloro-4-iodo, 2-bromo-4-iodo and 2-bromo-4-chloro-1,3,5-trineopentyl-benzene was studied by proton magenetic resonance measurements at 60 MHz. The identification of the lines of the AB quartets at low temperature was carried out on an HA-100 spectrometer by means of the INDOR technique. The activation parameters for all three barriers in each compound were found to be approximately the same, which perhaps reflects the interdependence of the rotations, with the smaller of the two halogens determining the size of the barrier. An explanation in terms of magnetic nonequivalence induced in the 1- and 5-methylenes by the 3-neopentyl group is considered to be most plausible.     

An yttrium Mξ source for ESCA

A new source for producing YMξ radiation in an ESCA spectrometer is described. The system makes use of continuous evaporation of yttrium on a rotating anode. It is demonstrated that this scheme allows YMξ-excited electron spectra to be recorded without gradual loss of resolution and intensity due to anode oxidation. Electron spectra of Ar, Hg and N₂ excited by YMξ radiation are studied. Relative photoelectric cross-sections of the 5d_{$\text{5}\text{2}$}, 5d_{$\text{5}\text{2}$} and 6s orbitals in Hg and the four valence orbitals in N₂ are measured. The valence electron shake-up spectrum of N₂ is discussed.