Studies on proton pump inhibitors. I. Synthesis of 8-[(2-benzimidazolyl)sulfinyl]-5,6,7,8-tetrahydroquinolines and related compounds

Many 8-[(2-benzimidazolyl)sulfinyl]-5,6,7,8-tetrahydroquinolines were synthesized and examined for their (H+ + K+) adenosine triphosphatase ATPase-inhibitory and antisecretory activities. These sulfinyl compounds could be considered to be rigid analogues of the 2-[(2-pyridyl)methylsulfinyl]benzimidazole class of antisecretory agents. All the compounds tested were potent inhibitors of (H+ + K+)ATPase. Most of the compounds also inhibited histamine-induced gastric acid secretion in rats. Among them, 8-[(5-fluoro-2-benzimidazolyl)sulfinyl]-3-methyl-5,6,7,8-tetrahydroqu inoline (XIVm) was found to have the most potent activity. The structure-activity relationships are discussed.     

Plutonium concentration and <Superscript>240</Superscript>Pu/<Superscript>239</Superscript>Pu isotopic ratio in the surface soils from the Jiuquan region in northwestern China

Surface soil samples collected in the Jiuquan region in the downwind area of the Chinese nuclear test site (CNTs) were analyzed for Pu isotopes. The ^239+240Pu activities ranged from 0.025 ± 0.009 to 0.89 ± 0.16 mBq g^?1, varying significantly with different sampling sites. The Dunhuang city that is located in the southwestern part of the Jiuquan region received the heaviest Pu deposition (^239+240Pu activities, 0.23–0.89 mBq g^?1). Most of the ²⁴⁰Pu/²³⁹Pu isotopic ratios were similar with that of the global fallout. However, the low values (0.080–0.147) observed in three sampling sites further supported the finding of Pu originated from CNTs in that region.     

Spin-density wave near the vortex cores in the high-temperature superconductor Bi2Sr2CaCu2O8+y

Competition with magnetism is at the heart of high-temperature superconductivity, most intensely felt near a vortex core. To investigate vortex magnetism we have developed a spatially resolved probe based upon NMR spin-lattice-relaxation spectroscopy. With this approach we have found a spin-density wave associated with the vortex core in Bi(2)Sr(2)CaCu(2)O(8+y), similar to checkerboard patterns in the local density of electronic states reported from scanning tunneling microscope experiments. We have determined both the spin-modulation amplitude and decay length from the vortex core in fields up to H=30 T.     

Pressure loading of detonation waves through 90-degree bend in high pressure H2–O2–N2 mixtures

Detonation experiments are conducted to investigate the detonation wave behavior in steam pipelines of boiling water reactors. Accumulated gases in BWRs are stoichiometric hydrogen/oxygen mixtures diluted with steam at 7 MPa. In the experiment, flammable gas mixture diluted with nitrogen at room temperature and up to 5 MPa is used to achieve equivalent detonation condition. Two test pieces are used, one is straight tube and the other is 90-degree bend. No initial pressure dependency in detonation wave behavior is observed in the experiments. However, in the straight tube tests, detonation velocities higher than theoretical values are measured when the initial pressures are greater than 2.3 MPa. This result is considered as attribution of real gas effect. In the 90-degree bend experiments, pressure time histories reveal pressure loads greater than the straight tube portion at two locations. One is a high pressure peak at the extrados of the bend and the other is a double pressure peak just downstream of the bend outlet. Second pressure peak just downstream of the bend outlet is due to transverse wave propagation. Additionally, the largest impulse is observed not at the extrados of the bend but at the intrados of bend outlet. These results show the importance of more investigations on transverse wave behaviors in failure potential evaluation.     

Apparent diffusion coefficient of line scan diffusion image in normal prostate and prostate cancer—comparison with single-shot echo planner image

Purpose

This retrospective study was designed to evaluate the apparent diffusion coefficient (ADC) of line scan diffusion images (LSDI) in normal prostate and prostate cancer. Single-shot echo planner images (SS-EPI) were used for comparison.

Materials and Methods

Twenty prostate tumors were examined by conventional MRI in 14 patients prior to radical prostatectomy. All patients were examined with a 1.5-T MR imager (Signa CV/i ver. 9.1 GE Medical System Milwaukee, WI, USA). Diffusion-weighted MR imaging (DWI) using LSDI was performed with a pelvic phased-array coil, with b values of 5 and 800 s/mm². DWI using SS-EPI was performed with a body coil, with b values of 0 and 800 s/mm². The ADCs of each sequence for 14 normal prostate and 20 prostate cancers were histopathologically assessed. Signal-to-noise ratio (SNR) on DWI was estimated and compared for each sequence.

Results

The mean ADCs (±S.D.) of normal peripheral zones (PZ), transition zones (TZ) and cancer (in 10⁻³ mm²/s) that used LSDI were 1.42±0.12, 1.23±0.10 and 0.79±0.19, respectively. Those that used SS-EPI were 1.76±0.26, 1.38±0.20 and 1.05±0.27, respectively. Using unpaired t test (P<.05), we found a significant difference in each sequence between normal tissue (both PZ and TZ) and the cancer. Paired t test (P<.05) also registered a significant difference between LSDI and SS-EPI. Mean SNR for DWI using LSDI was 16.49±5.03, while the DWI using SS-EPI was 18.85±9.26. The difference between the SNR of each sequence was not statistically significant by paired t test.

Conclusion

We found that ADCs using LSDI and SS-EPI showed similar tendencies in the same patients. However, in all regions, LSDI ADCs had smaller standard deviations than SS-EPI ADCs.     

Development of ion transportation, extraction and neutralization systems for atomic beam resonance method

A device that produces a low-energy and largely spin polarized RI beam based on the atomic beam resonance method (RIABR) has been developed. We have performed measurements of stopping and drifting an incoming RI ion beam in a gas chamber, extraction of the ions into a vacuum region, and neutralization of the extracted low-energy ion beam. The drift efficiency of RI ions in a gas and the extraction efficiency at a Laval-type glass nozzle were found to be 0.72±0.04 and 0.033, respectively. The result of the experiment for the neutralization is also discussed.     

Utility of mixture of commercially available polymers as constituents of sustained-release microcapsules containing cefadroxil or theophylline.

Hydroxy propyl methyl cellulose acetate succinate high grade (AS-HG) and ethyl cellulose (EC) mixture microcapsules containing cefadroxil or theophylline were prepared by a solvent evaporation method in liquid paraffin dissolved sorbitan tri-stearate as a dispersing agent, and their sustained-release properties were evaluated. The microcapsules prepared with AS-HG:EC (in a 2:5 weight ratio) mixture containing 20% of cefadroxil or theophylline exhibited apparent zero-order releasing pattern in pH 6 to 8, at 50 rpm and 37 degrees C (paddle method). These microcapsules were administered orally to beagle dogs and the plasma concentrations of cefadroxil or theophylline were measured periodically. As a result of in vivo investigation, a satisfactory sustained-release plasma pattern and an apparent zero-order process in the gastrointestinal absorption were confirmed by deconvolution analysis of both drugs.     

Total Synthesis of Proposed Structure of Yuremamine and All Diastereomers Using [3+2]‐Cycloaddition of Platinum‐Containing Azomethine Ylide

Total synthesis of the proposed structure of yuremamine has been achieved for the first time based on the intermolecular [3+2]‐cycloaddition reaction of the platinum‐containing azomethine ylide. All the possible diastereomers of yuremamine were also synthesized via the common intermediate. Through these syntheses, it was confirmed that the proposed structure of yuremamine and the diastereomers differ from the natural product.     

Highly selective photoinduced perfluoroalkylation of vinylsilanes and its application to synthesis of water-shedding polysilanes

The functionalization of polysilanes is an important subject in materials science because functionalized polysilanes are expected to exhibit potentially innovative properties. This research aims at the addition of a water-shedding property to polysilanes by introducing perfluoroalkyl groups into their skeleton. The photoinduced iodoperfluoroalkylation of various vinylsilanes takes place successfully upon irradiation with a xenon lamp: vinylmonosilanes undergo iodoperfluoroalkylation with perfluoroalkyl iodides (R_fI) regioselectively, and the corresponding perfluoroalkylated silanes are obtained in moderate to high yields. Detailed optimization of the photoinduced iodoperfluoroalkylation has been investigated to apply this method to the functionalization of polysilanes. Polysilanes having vinyl groups can be synthesized by the reductive coupling of dichlorovinylsilanes with samarium diiodide (SmI₂) and samarium metal (Sm) upon irradiation with visible light. The synthesized vinylpolysilanes and R_fI (about 1.0 mM CHCl₃ solution) are coated on a glass plate sequentially, and then the following photoirradiation with light of a wavelength over 300 nm successfully adds an excellent water-shedding property to the glass plate.     

Reversible photocontrol of surface wettability between hydrophilic and superhydrophobic surfaces on an asymmetric diarylethene solid surface

By alternate UV and visible light irradiation, reversible topographical changes were observed on a newly synthesized diarylethene microcrystalline surface between the rough crystalline surface of an open-ring isomer and flat eutectic surfaces. The contact angle changes of a water droplet between 80° and 150° and peak intensities changes of the open-ring isomer in XRD patterns within 2 h of repeating cycle were observed. The results indicated that reversibly photogenerated rod-shaped crystals on the surface were produced based on the lattice of the open-ring isomer crystals in the subphase.