4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist

A novel series of benzoic acid derivatives as VLA-4 antagonists were synthesized. Optimization, focusing on activity and lipophilicity needed for cell permeability, resulted in the identification of 15b and 15e with good activity (IC50 = 1.6 nM each) and moderate lipophilicity (Log D = 2.0, 1.8). Furthermore, 15e demonstrated efficacy in murine asthma model by an oral dose of 30 mg/kg.     

Capillary electrophoretic discrimination of single nucleotide polymorphisms using an oligodeoxyribonucleotidepolyacrylamide conjugate as a pseudo-immobilized affinity ligand: optimum ligand length predicted by the melting temperature values.

We developed a weak-affinity separation system for single-nucleotide polymorphisms (SNPs) based on capillary electrophoresis. In this approach, single-stranded DNA (ssDNA)-polyacrylamide (polyAAm) conjugate was used as a pseudo-immobilized affinity ligand to separate the target DNA, cytochrome P450 2C9 (CYP2C9), and its point mutant. The ligand DNA was designed to be complementary to the normal DNA, and the target DNA was electrophoretically separated by the difference in the affinity with the pseudo-immobilized ligand in the capillary. We showed that the separation efficiency was closely associated with the Tm value of double-stranded DNA (dsDNA) consisting of the target and ligand DNA, which depends on the measurement conditions, such as the base number of the ligand DNA and the concentration of Mg2+ in the buffer solution.     

Prediction of carcinogenicity of polynuclear aromatic hydrocarbons on the basis of their chemical structures

The carcinogenicities of polynuclear aromatic hydrocarbons in particulates extracted from diesel engine exhaust are predicted on the basis of the combined bay-L region theory proposed earlier, in conjunction with pattern recognition techniques. The predicted carcinogenicities agree well with experimental data, thus showing the validity of the proposed model equations.     

Railgun using plasma initiation separated from the projectile

Preacceleration of a projectile is important for reducing the erosion of the bore surface in a railgun. Gas guns, electrothermal guns, and other railguns are commonly used to preaccelerate the projectile. A new method, called the plasma initiation separated from the projectile (PISP) method is proposed, and its effectiveness is confirmed experimentally. A thin copper wire is placed near the edge of the railgun, and it explodes and forms a plasma that has a fast flow velocity due to the Lorentz force. This fast flowing plasma collides with the projectile, which obtains an initial velocity mainly by the momentum transfer. Since the current increases while only the plasma is accelerated, the driving force of the projectile just after the collision of the plasma with the projectile is large. The PISP method works as an inductive energy storage circuit with an opening switch     

Spectral Gap and Exponential Decay of Correlations

We study the relation between the spectral gap above the ground state and the decay of the correlations in the ground state in quantum spin and fermion systems with short-range interactions on a wide class of lattices. We prove that, if two observables anticommute with each other at large distance, then the nonvanishing spectral gap implies exponential decay of the corresponding correlation. When two observables commute with each other at large distance, the connected correlation function decays exponentially under the gap assumption. If the observables behave as a vector under the U(1) rotation of a global symmetry of the system, we use previous results on the large distance decay of the correlation function to show the stronger statement that the correlation function itself, rather than just the connected correlation function, decays exponentially under the gap assumption on a lattice with a certain self-similarity in (fractal) dimensions D < 2. In particular, if the system is translationally invariant in one of the spatial directions, then this self-similarity condition is automatically satisfied. We also treat systems with long-range, power-law decaying interactions.     

Measurement of Principal-Stress Directions from Photoelastic Experiment Using Generalized Phase-Shift Method

A generalized phase-shift method is developed for automatic measurement of principal-stress directions in the whole field of a model from photoelastic experiments. This method uses a set of light intensities obtained from the rotation of polaroids in dark-field plane polariscopes at each point. To investigate the accuracy of the measurement, time-series light intensity curves with different noise and different numbers of data which constitute the curves are used in computer simulation. The error of the measurement of the principal-stress directions obtained by the method is not greatly affected by noise when the number of data exceeds 50. This method is applied to a circular disk subjected to a concentrated load. The principal-stress directions obtained by the method are found to be in good agreement with the theory.Presented at 1996 International Workshop on Interferometry (IWI ‘96), August 27–29, Saitama, Japan.     

Performance Change of the Oxidative Coupling of Methane Induced by the Modification Effect of Lithium on a Mn-Mg-O Solid Solution

Lithium made a Mn-Mg-O solid solution stable upon exposure of methane, decreased the ethane and ethylene formation rates, and increased the COx formation rate during the oxidative coupling of methane. On the other hand, on MgO, lithium inhibited COx formation markedly and enhanced the selectivity of ethane 47% to 76%.