Syntheses and antiulcer activities of 2-aminonorbornene derivatives.

2,2,-Disubstituted norbornenes (1, 2), 2,2-Disubstituted norbornane (3), 2,2,3-trisubstituted norbornenes (4, 5), oxanorbornenes (6) and azanorbornenes (7) were synthesized by the Diels-Alder reaction using alpha, beta-dehydroamino acids as a key step, and their antiulcer activities were examined. The oxazolidine derivative (1h) exhibited the most potent activities against several ulcer-models in rat.     

Femtosecond Diffuse-Reflectance Spectroscopy of Various Commercially Available TiO2 Powders

The transient absorption properties of several commercially available TiO₂ photocatalysts were investigated by femtosecond diffuse-reflectance spectroscopy. Using femtosecond diffuse-reflectance spectroscopy, the quantities and rates of the initial trapping processes of holes and electrons generated by the photoexcitation of TiO₂ photocatalysts were investigated. It was found that the total amounts of trapped electrons for the pure-anatase and pure-rutile TiO₂ became smaller with increasing particle size, but increased again when the particles’ diameters were larger than 50 nm. The anatase–rutile mixed TiO₂ photocatalysts were found to have smaller amounts of trapped electrons compared with pure-anatase and pure-rutile TiO₂ photocatalysts. The lifetimes of trapped holes of various TiO₂ photocatalysts were also investigated, and it was found that the lifetimes were proportional to the anatase–rutile mixed ratios.     

On homotopy groups of quandle spaces and the quandle homotopy invariant of links

For a quandle X, the quandle space BX is defined, modifying the rack space of Fenn, Rourke and Sanderson (1995) [13], and the quandle homotopy invariant of links is defined in Z[π₂(BX)], modifying the rack homotopy invariant of Fenn, Rourke and Sanderson (1995) [13]. It is known that the cocycle invariants introduced in Carter et al. (2005) [3], Carter et al. (2003) [5], Carter et al. (2001) [6] can be derived from the quandle homotopy invariant.In this paper, we show that, for a finite quandle X, π₂(BX) is finitely generated, and that, for a connected finite quandle X, π₂(BX) is finite. It follows that the space spanned by cocycle invariants for a finite quandle is finitely generated. Further, we calculate π₂(BX) for some concrete quandles. From the calculation, all cocycle invariants for those quandles are concretely presented. Moreover, we show formulas of the quandle homotopy invariant for connected sum of knots and for the mirror image of links.     

Pharmazeutische Pr?parate

Ohne Zusammenfassung     

Studies on sesquiterpenoids—III Some derivatives of guaiol

When guaiol was dehydrated with such reagents as thionyl chloride-pyridine, phosphorus oxychloride-pyridine or potassium bisulphate, the isopropenyl derivative (IIa) was always obtained as a main product, together with a small amount of IIb. Catalytic reduction of IIa in alkaline media afforded -dihydroguaiene (V), while in neutral or acid media it gave a mixture of V and its double bond isomer (VI).     

Solid-phase syntheses of olefin-containing inhibitors for HTLV-1 protease using the Horner-Emmons reaction

[reaction: see text] The solid-phase Horner-Emmons reaction was successfully applied for the convenient syntheses of olefin-containing protease inhibitors. The isomerization during the solid-phase Horner-Emmons reaction can be minimized simply by the use of an appropriate amount of the base. The synthesized olefin peptides, which have an olefin gamma-amino acid at the scissile site, were found to act as effective inhibitors for the HTLV-1 protease for the first time.     

Sesquiterpenoids and flavonoids from the aerial parts of Tithonia diversifolia and their cytotoxic activity

Cytotoxicity-guided fractionation of the 80% EtOH extract of Tithonia diversifolia has resulted in the isolation of twelve sesquiterpenoids (1-12), including three new ones (4, 10, 12), and three known flavonoids (13-15). The structures of the new compounds were determined by analysis of their spectroscopic data. The isolated compounds showed cytotoxic activity against HL-60 leukemia cells with IC(50) values ranging from 0.13 to 13.0 microM, when etoposide used as a positive control gave an IC(50) value of 0.43 microM. The cancer growth inhibitory property of 9, the main cytotoxic compound in T. diversifolia, was examined using a disease-oriented panel composed of 39 human cancer cell lines in the Japanese Foundation for Cancer Research.