Synthesis and evaluation of 6-nitro-7-(1-piperazino)quinazolines: dual-acting compounds with inhibitory activities toward both tumor necrosis factor-alpha (TNF-alpha) production and T cell proliferation

We investigated the chemical modifications of the nitroquinazoline derivative (1) through the replacement of the NH group at the C(4)-position with several N-alkyl groups to increase the lipophilicity at the C(4)-position. Among them, we found that the N-methyl analogue (5a) showed a 2-fold loss in the inhibitory activity toward tumor necrosis factor-alpha (TNF-alpha) production in vitro as compared with the NH analogue (1); however, 5a exhibited an oral inhibitory activity on TNF-alpha production with an ED50 value of 26 mg/kg, whereas 1 did not. Moreover, the oral bioavailability of 5a was higher than that of 1 (1, F=1%; 5a, F=21%), and the calculated ClogP value for 5a was higher than that for 1. These results suggest that the improved lipophilicity of 5a compared with that of 1 reflects its greater inhibitory activity on TNF-alpha production in vivo as well as oral bioavailability.     

Formation,structure, and structural properties of a new filamentary tubular form: hollow conical-helix of graphitic boron nitride

A novel tubular form of graphitic boron nitride (BN) displaying a hollow conical-helix was discovered. It was generated via wrapping a single beltlike filament according to the geometry of an Archimedes spiral. Cone apex angles of helical-conical nanotubes (HCNTs) were found to exhibit specific values, each of which refers to a certain coincidence site lattice. A unique structural property of HCNTs was observed, displaying the transformation of apex angles during the annealing process. The observed apex angles were reduced with decreasing annealing temperature, which is in accordance with an estimated HCNT strain energy decrease for a given tubular radius. It is suggested that the curvature and apex angle of a HCNT are determined by a sole dynamic element, that is, enthalpy (DeltaH), whereas the HCNT disclination configuration changes through helical sliding of the filament.     

Unprecedented hydrothermal reaction of o-phenylaniline and related derivatives with cyclic ketones. A novel approach to the construction of phenanthridine and quinoline ring systems

[reaction: see text] A new method for synthesizing phenanthridine and its related compounds was developed using the condensation of o-phenylaniline and its homologues with cyclic ketones under hydrothermal conditions.     

Good ideals in Gorenstein local rings

Let be an -primary ideal in a Gorenstein local ring (, ) with , and assume that contains a parameter ideal in as a reduction. We say that is a good ideal in if is a Gorenstein ring with . The associated graded ring of is a Gorenstein ring with if and only if . Hence good ideals in our sense are good ones next to the parameter ideals in . A basic theory of good ideals is developed in this paper. We have that is a good ideal in if and only if and . First a criterion for finite-dimensional Gorenstein graded algebras over fields to have nonempty sets of good ideals will be given. Second in the case where we will give a correspondence theorem between the set and the set of certain overrings of . A characterization of good ideals in the case where will be given in terms of the goodness in their powers. Thanks to Kato's Riemann-Roch theorem, we are able to classify the good ideals in two-dimensional Gorenstein rational local rings. As a conclusion we will show that the structure of the set of good ideals in heavily depends on . The set may be empty if , while is necessarily infinite if and contains a field. To analyze this phenomenon we shall explore monomial good ideals in the polynomial ring in three variables over a field . Examples are given to illustrate the theorems.

     

Finite Modules of Finite Injective Dimension Over a Noetherian Algebra

Let R be a commutative Noetherian ring. Let P(R) (respectively,I(R)) be the category of all finite R-modules of finite projective(respectively, injective) dimension. Sharp [9] constructed acategory equivalence between I(R) and P(R) for certain Cohen–Macaulaylocal rings R. Thus many properties about finite modules offinite projective dimension can be connected with those of finiteinjective dimension through this equivalence.     

Solubilization of C60 by micellization with a thermoresponsive block copolymer in water: Characterization,singlet oxygen generation,and DNA photocleavage

Water‐soluble diblock copolymer, poly(N‐isopropylacrylamide)‐block‐poly(N‐vinyl‐2‐pyrroridone) (PNIPAM_m‐b‐PNVP_n), was found to associate with fullerene (C₆₀), and thus C₆₀ can be solubilized in water. The 63C₆₀/PNIPAM_m‐b‐PNVP_n micelle formed a core‐shell micelle‐like aggregate comprising a C₆₀/PNVP hydrophobic core and a thermoresponsive PNIPAM shell. The C₆₀‐containing polymer micelle formation and its thermoresponsive behavior were characterized using light scattering and ¹H NMR techniques. The hydrodynamic radius (R_h) of the C₆₀‐bound polymer micelle increased with increasing temperature, which was ascribed to the hydrophobic association between dehydrated PNIPAM shells above lower critical solution temperature (LCST). ¹H NMR data suggest that the motion of the PNIPAM block is restricted above LCST due to the dehydration of the PNIPAM shell in water. The generation of singlet oxygen by photosensitization by the C₆₀‐bound polymer micelle was confirmed from photooxidation of 9,10‐anthracenedipropionic acid. Furthermore, DNA was found to be cleaved by visible light irradiation in the presence of the C₆₀‐bound polymer micelle. Therefore, there may be a hope for a pharmaceutical application of the C₆₀‐bound polymer micelle to cancer photodynamic therapy. © 2011 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2011.     

Synthesis and isomerization of conjugated oligomers containing azoimidazole unit

The Suzuki (for O1 – O3 ) and Stille (for O4 ) coupling polymerization of 2‐(phenylazo)imidazole bearing the benzyl protecting group at the 1‐position gave conjugated oligomers. The transformation from the neutral imidazole in the conjugated oligomer O2 , consisted of the alternating 2,5‐didecyl‐1,4‐phenylene unit, to the cationic imidazolium salt O2S was performed. Depending on the chemical structure of coupling partners, the absorption maximum of conjugated oligomers showed red shift or blue shift from that of the model compound M with the benzene ring at the 4,5‐positions. The absorption maximum wavelength of the cationic conjugated oligomer O2S showed a blue shift from that of the neutral conjugated oligomer O2 . The trans‐to‐cis photoisomerization of the azoimidazole unit in conjugated oligomers was observed by irradiating the light at 436 nm, and the conversion degree to the cis structure had a rough correlation with the maximum absorption wavelength of materials. The trans‐to‐cis photoisomerization in the film state was sluggish. On the other hand, the cis‐to‐trans thermal isomerization of the azoimidazole unit was confirmed and the absorbance returned to the initial state before the photoisomerization. The trans‐to‐cis photoisomerization of the cationic conjugated oligomer O2S required large energy, and the prolonged light irradiation might decompose the azoimidazole unit. © 2011 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2011.     

Wave propagation in saturated ground using the volume fractions

The purpose of this paper is to study the dynamic behavior of soft ground including a porous layer by considering the porosity change. In order to take the porosity change into account, the concept of the volume fraction, which has been proposed in continuum mechanics, is introduced. The constitutive equations presented by Bowen are applied to the analysis of the porous media. According to Bowen's theory, the porosity is considered as a variable called the volume fraction and has its own constitutive equation. The constitutive equation of the volume fraction has thermoelastic equation coefficients and is determined by the strains of the solid and the fluid. This means that the compressibilities of the solid and the fluid are considered. When the special condition is assumed, Bowen's theory can contain Biots's theory, which has been applied in earthquake engineering. The wave propagation in the ground including a porous layer, modeled by Bowen's theory, is studied and compared with that of Biot's theory. One-dimensional attenuation and surface amplitude are calculated. The effect of the volume fraction is discussed with respect to the compressibilities of the solid and the fluid.