A potent and highly selective sulfotransferase inhibitor

In the present work, we have used a newly developed, fluorescence-based assay to screen a library of >30 000 compounds as potential beta-arylsulfotransferase-IV inhibitors. A total of 11 inhibitors were discovered. Most of the compounds discovered showed low micromolar inhibition, but one of the compounds showed potent inhibition (Ki = 96 nM). The most potent of these inhibitors was tested against a variety of other purine binding enzymes and showed remarkable specificity.     

Intramolecular charge transfer with the planarized 4-aminobenzonitrile 1-tert-butyl-6-cyano-1,2,3,4-tetrahydroquinoline (NTC6)

Fast and efficient intramolecular charge transfer (ICT) and dual fluorescence is observed with the planarized aminobenzonitrile 1-tert-butyl-6-cyano-1,2,3,4-tetrahydroquinoline (NTC6) in a series of solvents from n-hexane to acetonitrile and methanol. Such a reaction does not take place for the related molecules with 1-isopropyl (NIC6) and 1-methyl (NMC6) groups, nor with the 1-alkyl-5-cyanoindolines with methyl (NMC5), isopropyl (NIC5), or tert-butyl (NTC5) substituents. For these molecules, a single fluorescence band from a locally excited (LE) state is found. The charge transfer reaction of NTC6 is favored by its relatively small energy gap DeltaE(S(1),S(2)), in accordance with the PICT model for ICT in aminobenzonitriles. For the ICT state of NTC6, a dipole moment of around 19 D is obtained from solvatochromic measurements, similar to micro(e)(ICT) = 17 D of 4-(dimethylamino)benzonitrile (DMABN). For NMC5, NIC5, NTC5, NMC6, and NIC6, a dipole moment of around 10 D is determined by solvatochromic analysis, the same as that of the LE state of DMABN. For NTC6 in diethyl ether at -70 degrees C, the forward ICT rate constant (1.3 x 10(11) s(-1)) is much smaller than that of the back reaction (5.9 x 10(9) s(-1)), showing that the equilibrium is on the ICT side. The results presented here make clear that ICT can very well take place with a planarized molecule such as NTC6, when DeltaE(S(1),S(2)) is sufficiently small, indicating that a perpendicular twist of the amino group relative to the rest of the molecule is not necessary for reaching an ICT state with a large dipole moment. The six-membered alicyclic ring in NMC6, for example, prevents ICT by increasing DeltaE(S(1),S(2)) relative to that of DMABN.     

Functions of translation type and functorial properties of Segal algebras II

In this paper we investigate functorial properties of the Segal algebra which consists of all functionsf in Wiener's algebra onG with Fourier transform in Wiener's algebra on the dual group . Especially may serve as a very large and natural domain for Poisson's formula. Moreover, there is introduced a Segal algebraE ₀(G) containing as a subspace, but still eachfE ₀(S) satisfies Poisson's formula.     

Low distortion recording of transient low- light-level phenomena

Two types of low-light-level image sensors have been investigated for use in low distortion recording: an SIT-vidicon (Silicon-Intensifier Target), and a sensor consisting of a newvicon and two stage proxifier. The results are compared and discussed. In addition, a triggerable video frame store is described.     

Al-Mn-Ce quasicrystalline composites: Phase formation and mechanical properties

Aluminium-based composites with quasicrystalline particles as reinforcements were synthesized via the powder metallurgy processing route. In order to obtain bulk samples with a nanoscale microstructure most equivalent to that resulting from rapid solidification, powders of Al-Mn-Ce alloys were prepared by pulverization of melt-spun ribbons using a planetary ball mill. Significant differences in the phase formation upon quenching, composite microstructure and thermal stability of the microstructure were found for different alloy compositions. Severe grain growth during the subsequent consolidation by hot extrusion caused the formation of a micrometre-scale composite instead of the nanoscale phase mixture initially existing after rapid solidification. After hot extrusion, the specimens were deformed by compression at a constant compression rate at room temperature. With an ultimate strength of up to 975 MPa and a ductility of more than 4% the material yields excellent properties compared with conventionally produced aluminium-based alloys.     

Electron energy-loss spectroscopy at incommensurately modulated crystalline and glassy Ba2TiGe2O8

Based on cluster molecular orbital calculations, high-energy resolution (ΔE?～ 0.4?eV) Ti–L_2,3 electron energy loss near-edge structures of single-crystalline and glassy Ba₂TiGe₂O₈ are interpreted. The finding that the Ti–L_2,3 near-edge structure of the Ba₂TiGe₂O₈ single crystal possesses less pronounced peaks than the glass under identical experimental conditions can be attributed to distinct distortions of the titanium environment caused by the very strong one-dimensional structural modulation hosted by the Ba₂TiGe₂O₈ crystal lattice. As lattice periodicity is absent in the glass, the titanium environment is more regular in the vitreous surroundings. Moreover, the modulation in crystalline Ba₂TiGe₂O₈ is responsible for the virtually indiscernible O–K near-edge structures of the glassy and crystalline samples.