Synthesis and antibacterial activity of new 1beta-methylcarbapenems having the potential for intramolecular nonbonded S...O interactions.

Mercaptoacetyliminothiadiazoline derivatives (19, 20) useful for the pendant moiety of 1beta-methylcarbapenem antibiotics were efficiently synthesized. Acetyl derivative (18) of 20 was submitted to X-ray analysis, and a significant nonbonded S...O close contact was recognized in the crystallographic structure. New 1beta-methylcarbapenems (5, 6) were synthesized by exploiting 19 and 20, and exhibited considerable antibacterial activities in vitro.     

Finsler Hardy inequalities

In this paper we present a unified simple approach to anisotropic Hardy inequalities in various settings. We consider Hardy inequalities which involve a Finsler distance from a point or from the boundary of a domain. The sharpness and the non-attainability of the constants in the inequalities are also proved.     

Coulomb and strong interactions for Bose-Einstein correlations

We present an analytical formula for the Bose-Einstein correlations (BEC) which includes effects of both Coulomb and strong final state interactions (FSI). It was obtained by using Coulomb wave function together with the scattering partial wave amplitude of the strong interactions describing data on thes-wave phase shift. We have proved numerically that this method is equivalent to solving Schrödinger equation with Coulomb and thes-wave strong interaction potentials. As an application we have analysed, using our formula which includes the degree of coherence and the long range correlation, the data fore ⁺ e ^? annihilations. We have found that the degree of coherence present in our formula approaches approximately unity whereas the long range correlation parameter becomes approximately zero. These results suggest that the physical meanings of the fractional degree of coherence and the long range correlation observed in various other analyses can most probably be attributed to FSI.     

Morphology control of polypropylene by crystallization under carbon dioxide

We investigated the crystalline morphology of isotactic polypropylene obtained by melt crystallization under carbon dioxide (CO₂) at various pressures. Spherulites consisting of regularly arranged fibrils without subsidiary lamellae were obtained by crystallization under CO₂ below 2 MPa, whereas large spherulites consisting of irregularly arranged fibrils with subsidiary lamellae were obtained under ambient pressure. Distorted domain crystals with uniform optical anisotropy consisting of α‐form were found to be obtained under CO₂ above 2 MPa, and needle crystals consisting of γ‐form were obtained above 12 MPa. Transmission electron micrographs showed that straight and thick lamellae are regularly arranged in both the distorted domain crystals and the needle crystals. The uniformly thick lamellae were confirmed by differential scanning calorimetry thermograms; that is, the melting temperature is higher and the melting peak is sharper than those obtained under ambient pressure. Such characteristic crystalline morphologies obtained under CO₂ may be attributed to local ordering in the melt state. © 2004 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys 42: 2738–2746, 2004     

Application of in vivo ESR spectroscopy to pharmaceutical sciences: Evaluation of in vivo inhibitory mechanism of antigastric lesion drugs

In order to analyze free radical reactions in living stomach, we developed a noninvasive measurement by an in vivo electron spin resonance (ESR) and spin probe technique and applied it to mucosal injury. NH₄OH-induced gastric lesions were prepared in rats. A nitroxyl probe was administered intragastrically or intravenously, and then in vivo ESR spectra of the gastric region were obtained by 300 MHz ESR spectroscopy. The signal of the intragastrically administered spin probe decreased gradually and the decay significantly enhanced 30 min after NH₄OH administration. The enhanced signal decay was attributed to the OH radical generation, since it was completely suppressed by mannitol, catalase, and desferrioxamine. Two commercially available antigastric lesion drugs, rebamipide and taurine, were tested with a NH₄OH-induced gastric lesion model. Both intraperitoneal administration of rebamipide and intravenous administration of taurine suppressed gastric lesion formation induced by NH₄OH in a dose-dependent manner. Intraperitoneal preadministration of rebamipide also suppressed the enhanced signal decay, but neither pre- nor coadministration of taurine showed any effect on the enhanced signal decay. The results strongly indicate that the inhibitory mechanism on gastric lesion formation in NH₄OH-treated rats is quite different for the two antigastric lesion drugs rebamipide and taurine.     

Fluorimetric determination of oleandomycins with nicotinamide and 3-acetylpyridine

The method is based on a fluorescence reaction of the epoxy group with nicotinamide and 3-acetylpyridine. Oleandomycin phosphate and triacetyloleandomycin can be determined in the ranges 1–80 μg ml^?1and 5–80 μg ml^?1, respectively, with relative standard deviations of 3–5%. The method can be applied to pharmaceutical preparations. Results obtained by this method and by bioassay in an examination of residual potency agreed well when degradation was done under neutral or alkaline conditions.