WSS2220, a novel cyclic tetrapeptide with a new sulfonoamino acid, exhibits potent and selective inhibitory activity against GlyT1

In the course of our screening program for novel glycine transporter inhibitors, we obtained a novel cyclic tetrapeptide (WSS2220) from the culture broth of Nonomuraea sp. The structure of WSS2220 was elucidated based on physicochemical data. WSS2220 contained a novel amino acid (4-oxo-3′-sulfoisoleucine), the absolute stereochemistry of which was determined by chemical modifications and the modified Mosher’s method. WSS2220 selectively inhibited glycine transporter type1 with an IC₅₀ of 20 nM.     

Interaction among cluster in chalcogen-rich glasses of Ge1−x(S or Se)x

The composition and pressure dependence of Raman spectra and the optical gap is investigated in order to see interactions among clusters in chalcogen-rich Ge_1?x(S, or Se)_x glasses.     

Structure changes induced by external multiplicative noise in the electrohydrodynamic instability of nematic liquid crystals

We study the influence of external multiplicative noise on the electrohydrodynamic instability (EHD) in nematic liquid crystals. It turns out that the correlation time _n and the intensityQ of the noise are the crucial parameters to control the system. Different types of noise lead to minor quantitative changes when compared to Gaussian white noise, leaving the qualitative aspects unchanged. With increasing noise intensity the threshold for the onset of the first instability changes drastically. We observe that the curvature arising when the threshold of the various instabilities is plotted as a function of the noise intensity changes as one is going, e.g., from the onset of Williams domains (WD) to the onset of the grid pattern (GP). This result reflects the transition in the flow structure from two-dimensional (WD) to three-dimensional (GP, DSM) flow patterns. As the intensity of the noise is increased further, the onset of the first instability becomes more complex. The measurement of the nonlinear onset time shows a strong dependence on the noise intensityQ, which is linear for WD and GP well above onset. The linear onset time shows an unexpected dependence on the noise intensity close to the onset of the first instability. For sufficiently long correlation times of the noise, a destabilization by noise is obtained.     

Gas chromatography of dimethylalkylsilyl ether derivatives of bile acid methyl esters

The gas chromatographic separation of the DMAS ether derivatives of ten bile acid methyl esters, namely DMES, DMnPS and DMiPS ethers, have been studied by use of an open tubular glass capillary column, coated with SE-30. The DMAS ether derivatives were eluted in sequence according to the number of hydroxyl groups except for 12-KCDCA, and separated. This contrasts with the poorly resolved gas chromatographic peaks produced by the TMS ether derivatives. The DMES ether derivatives were resolved with baseline separation in 30 min, but those of HCA and 12-KCDCA had similar methylene unit values.     

Semi-quantitative method of N-isopropyl-(123I)-p-iodoamphetamine accumulation in cerebrum: cerebrum to cerebellum accumulation ratio

Semi-quantitative method of N-isopropyl-(123I)-p-iodoamphetamine (123I-IMP) accumulation in cerebrum by using 123I-IMP SPECT was tried. Ratio of counts in whole cerebrum to those in normal cerebellum was calculated, and this accumulation is defined as cerebrum to cerebellum accumulation ratio. In group of patients with dementia or patients who were remaining in bed, significantly low accumulation ratio was observed, while in "normal" group, no differences in sex and aging were observed. Calculation of cerebrum to cerebellum accumulation ratio was concluded as a useful method of evaluating the accumulation of 123I-IMP in cerebrum.     

Hydrogen‐bonded complexes of 2‐pyridone with centrosymmetric and non‐centrosymmetric dicarboxylic acids

2‐Pyridone (2‐oxo­pyrimidine) forms hydrogen‐bonded com­plexes with di­carboxyl­ic acids, the molar ratio of 2‐pyridone/di­carboxyl­ic acid being 2:1 for the complexes with oxalic acid (ethanedioic acid), 2C₅H₅NO·C₂H₂O₄, (I), and trans‐β‐hydro­muconic acid (trans‐hex‐3‐enedioic acid), 2C₅H₅NO·C₆H₈O₄, (II), and 1:1 for the complexes with trans‐glutaconic acid (trans‐pent‐2‐enedioic acid), C₅H₅NO·C₅H₆O₄, (III), and l ‐­tartaric acid (l ‐2,3‐di­hydroxy­butane­dioic acid), C₅H₅NO·C₄H₆O₆·H₂O, (IV). Common features in the hydrogen‐bonding patterns were found for the centrosymmetric and non‐centrosymmetric acids, respectively. The 2‐pyridone mol­ecule takes the lactam form in these crystals.     

Synthesis of 4,5-disubstituted-3-deoxy-d-manno-octulosonic acid (Kdo) derivatives

In this study, a new synthetic approach to 4,5-branched Kdo trisaccharides based on the common acceptor Kdo(α2-4)Kdo was developed. The synthesis of three types of 4,5-branched trisaccharides, Hep(α1-5)[Kdo(α2-4)]Kdo, Man(α1-5)[Kdo(α2-4)]Kdo, and GalNAc(α1-5)[Kdo(α2-4)]Kdo, was achieved in good yield and high α-selectivity.