Synthesis and pharmacological evaluation of 1-alkyl-N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents

We synthesized and evaluated inhibitory activity against T-type Ca(2+) channels for a series of 1-alkyl-N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that the isopropyl substituent at the benzylic position plays an important role in exerting potent inhibitory activity, and the absolute configuration of the benzylic position was found to be opposite that of mibefradil, which was first launched as a new class of T-type Ca(2+) channel blocker. Oral administration of N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]-1-[2-(3-methoxyphenyl)ethyl]piperidine-4-carboxamide (17f) lowered blood pressure in spontaneously hypertensive rats without inducing reflex tachycardia, an adverse effect often caused by traditional L-type Ca(2+) channel blockers.     

Chemical trend of Ln-M exchange couplings in heterometallic complexes with Ln = Gd, Tb, Dy, Ho, Er and M = Cu, V

The 4f-3d exchange couplings were definitively and precisely determined in the dinuclear complexes (Ln-M) involving double μ-oxo-bridges, by means of combined high-frequency electron paramagnetic resonance and pulsed-field magnetization techniques, revealing a monotonic decrease of ferromagnetic J(Ln-Cu) in the order of the atomic number, (64)Gd to (68)Er.     

Photocatalytic reduction of nitrobenzenes to aminobenzenes in aqueous suspensions of titanium(IV) oxide in the presence of hole scavengers under deaerated and aerated conditions

Photocatalytic reduction of nitrobenzenes to corresponding aminobenzenes in aqueous suspensions of titanium(IV) oxide (TiO(2)) containing hole scavengers under various conditions was examined. In photocatalytic reduction of m-nitrobenzenesulfonic acid (m-NBS) in the presence of formic acid (FA) under deaerated conditions, m-aminobenzenesulfonic acid (m-ABS) was produced almost quantitatively in acidic suspensions and high efficiency (>99%) in FA utilization as a hole scavenger was achieved. No re-oxidation of m-ABS occurred in acidic conditions both in the presence and absence of FA. The high yield of m-ABS was explained by strong ability of FA as a hole scavenger and possible repulsion of the reduced functional group (ammonium group, -NH(3)(+)) from the protonated, i.e., positively charged TiO(2) surface in acidic suspensions avoiding re-oxidation of m-ABS. Using TiO(2) samples of various physical properties, which had been synthesized by a solvothermal method and post-calcination at various temperatures, effects of physical properties of the TiO(2) samples on m-ABS yield were also investigated. A linear correlation between the amount of m-NBS adsorbed and the m-ABS yield was observed, suggesting that ability of TiO(2) for m-NBS adsorption is one of the key factors for effective photocatalytic reduction of m-NBS to m-ABS. This photocatalytic system can be applied for reduction of aminonitrobenzenes to corresponding diaminobenzenes (DAB) in the presence of oxalic acid as a hole scavenger. High yields of m-ABS and DAB were achieved even when the reactions were performed in the presence of oxygen.     

Adjoint-based exact Hessian computation

BIT Numerical Mathematics - We consider a scalar function depending on a numerical solution of an initial value problem, and its second-derivative (Hessian) matrix for the initial value. The need...     

Measurement of Reflected and Scattered Light for Monitoring Fluctuation of Structures

A laser spectroscopic technique for studying fluctuations of structural objects is presented, together with some results of our investigations including an observation of forced vibration of a refrigerator, intrinsic vibrations of buildings, and appearance of a fluctuation in rotational speed due to fatigue. An alternative detection technique which uses the scattered light for monitoring in place of the mirror-reflected beam is also presented. A leak of water out of a pipeline was detected with this method.

The results obtained with this laser spectroscopic technique should form a useful collection of data regarding fluctuation analysis of various objects.     

Investigation of muonic hydrogen isotopes scattering from H2 molecule

Hyperfine Interactions - Knowledge of the cross sections for scattering of µp, µd and µt on molecules of hydrogen isotopes is necessary not only for checking the algorithmic solution...     

Observation of phase transition of cesium manganese hexacyanoferrates by X-ray absorption spectroscopy

Cesium manganese hexacyanoferrates exhibit an interesting phenomenon of temperature-induced phase transition accompanied by a variation in the magnetic susceptibility. We observed the variation in the electronic state of Mn during the phase transition by using X-ray absorption spectroscopy. The results of the analyses showed that the content ratio of Fe^II-CN-Mn^III and Fe^III-CN-Mn^II systematically varied during the phase transition. However, the ratio of Fe^II-CN-Mn^II remained constant at almost all temperatures. These results suggest that the charge transfer between Fe and Mn ions in the Fe^III-CN-Mn^II or the Fe^II-CN-Mn^III bond produces the phase transition.     

Synthesis and characterization of crosslinked uniform polymeric microspheres containing a polyimide prepolymer by a new emulsification process

A highly crosslinked poly(styrene–divinyl benzene–trimethyolpropane trimethacrylate) microsphere containing a polyimide prepolymer (PIP) was prepared by a new emulsification method, Shirasu porous glass (SPG) membrane emulsification, and a subsequent radical suspension polymerization. That is, a mixture of styrene, divinyl benzene, trimethyol propane trimethacrylate (TMPTMA), and PIP containing an initiator was permeated through the uniform pores of the SPG membrane into a continuous phase containing a stabilizer to form uniform droplets. Then, the suspension polymerization was carried out at 65 °C for 24 h. The trifunctional crosslinker TMPTMA was added to enhance the destructive strength of the microsphere, and PIP was incorporated into the microsphere to provide an adhesion force by a known self‐curing reaction at 220 °C. The effects of the feed amounts of TMPTMA and PIP on the monomer conversion, size distribution, and destructive strength of the microsphere were investigated. The monomer conversion increased with an increase in TMPTMA. The particle size distribution became narrower as the TMPTMA feed amount increased, but it became broader with an increase in PIP. The destructive strength increased with increases in TMPTMA and PIP. After a heat treatment at 220 °C, the destructive strength decreased because of the heat degradation of the polymer. The addition of TMPTMA suppressed the heat degradation, and PIP could undergo self‐curing at 220 °C. The obtained highly crosslinked uniform microsphere containing PIP has potential applications in liquid‐crystal displays. © 2003 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 41: 2588–2598, 2003     

Preparation and characterization of single-phase SiC nanotubes and C-SiC coaxial nanotubes

Preparation conditions of single-phase SiC nanotubes and C-SiC coaxial nanotubes were investigated. The characterization of single-phase SiC nanotubes and C-SiC coaxial nanotubes were carried out. The SiC nanowires, which were made of the catenated SiC grains of 50–200 nm in diameter, were obtained in carbon nanotubes reacted at 1450 °C. The only C-SiC coaxial nanotubes were formed at 1300 °C. A few single-phase SiC nantoubes were synthesized at 1200 °C for 100 h. More than half number of nanotubes reacted at 1200 °C for 100 h were altered to single-phase SiC nantoubes by heat treatment of 600 °C for 1 h in air since the remained carbon was removed. The energy dispersive X-ray spectroscopy analysis revealed that the atomic ratio of Si to C in single-phase SiC nanotubes was almost 1; these single-phase SiC nanotubes consisted of near-stoichiometric SiC grains.