Condensed thienopyrimidines. II. Synthesis and gastric antisecretory activity of thiazole and polymethylene condensed thienopyrimidine derivatives

Thiazolo[3,2-a]thieno[3,2-d]-, [3,4-d]- and [2,3-d]pyrimidin-5-one derivatives (6, 11 and 16), and polymethylene condensed thieno[3,2-d]-, [3,4-d]- and [2,3-d]pyrimidin-5-one derivatives (19-21), in which the oxygen atom of the oxazolidine moiety in 3 was replaced by a sulfur atom or methylene groups, were synthesized and evaluated for gastric antisecretory activity in pylorus-ligated rats. The structure-activity relationships of these compounds are discussed.     

Alternating copolymers consisting of arylalkyl methacrylates. I. Fluorescence properties of poly(arylalkyl methacrylate-alt-styrene) in organic solution

Alternating and random copolymers of 9-phenanthrylmethyl methacrylate or 2-(9-carbazolyl)ethyl methacrylate with styrene were synthesized and their fluorescence properties were examined. There was no noticeable difference in the spectral features of the alternating and random copolymers in tetrahydrofuran (THF), demonstrating that this type of polymers have no quenching sites in the polymer chains. The fluorescence quenching studies indicated that the alternating copolymers permitted singlet-state energy migration as efficiently as the corresponding random copolymers but less efficiently than the random copolymers with higher chromophore contents. These results strongly suggest that to be chromophores close to each other is most important for facilitation of an intramolecular energy migration. © 1995 John Wiley & Sons, Inc.     

10B quantitative determination in ppb range by particle tracks reading for boron neutron capture therapy

Quantitative determination of ppb-order ¹⁰B was carried out in a small number of cultured tumor cells by particle tracks by the ₁₀B(n,)⁷Li reactions using solid state nuclear track detector (SSNTD) for boron neutron capture therapy research. The detection limit of ¹⁰B concentration in tumor cells is less than 1·10^-3 ppm under our experimental conditions which permits the quantitative determination of ¹⁰B in a small number of boronated tumor cells (10⁵/ml = ca. 0.1 mg). Boron quantities in tumor cells determined were well compatible with the tumor cell killing effects of boron neutron capture therapy.     

On the Theory of Gravitational Field in Finsler Spaces

Some structural considerations are made on the Finslerian gravitational field: A Finslerian metrical structure such as g_λχ(x, y) = γ_λχ(x) + h_λχ(x, y) is proposed, where γ_λχ denotes the Riemann metric of Einstein's gravitational field, while hλχ the Finsler metric induced by the Riemann metric h_ij(y) of the internal field; The intrinsic behaviour of the internal variable y, which is expressed as ?ⁱ = K(x, y) y^j in the internal field, is grasped by the Finslerian parallelism δyⁱ (=0), which is reflected in the spatial structure of the external gravitational field by the mapping relation δy^χ = e(x) δyⁱ. The whole metrical Finsler connection D for g_λχ(i.e., Dg_λχ = 0) is determined by taking account of the intrinsic behaviour δy^χ.     

Novel synthesis of macrocycles with 1,1′-binaphthalene-2,2′-diol using intramolecular oxidative coupling

A new series of BINOL-based macrocycles with two phenolic protons have been synthesized via oxidative coupling reaction using CuCl(OH)-TMEDA.     

Ca at C82 isomers: computed temperature dependency of relative concentrations

Relative concentrations of nine isomers of Ca at C82 derived from the C82 isolated-pentagon-rule satisfying cages are computed in a wide temperature interval. The computations are based on the Gibbs energy constructed from partition functions supplied with molecular parameters from density functional theory calculations. Five structures show significant populations at higher temperatures: C2v > Cs > C2 > C3v > Cs. The computed relative stabilities agree well with available observations.