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.     

Wave packet dynamics in a quasi-one-dimensional metal-halogen complex studied by ultrafast time-resolved spectroscopy

An ultrafast optical response is studied in a quasi-one-dimensional halogen-bridged mixed-valence metal complex [Pt(en)(2)] [Pt(en)2I2] (ClO4)(4) with ultrafast time resolution. Wave packet motions both in the ground and self-trapped exciton (STE) states are observed as oscillatory modulations in the time-resolved reflectivity. The wave packet motion on the STE potential surface begins after about 50 fs with respect to the photoexcitation. This delay is attributed to the lattice relaxation from the free exciton state to the STE state.     

22 dB all-fiber green amplifier using Er-doped fluoride fiber

We demonstrate a 22 dB all-fiber amplifier at 546 nm using Er³⁺-doped fluoride fiber by forward upconversion pumping of a 974 nm laser diode. The gain saturation effects and the power conversion efficiency of this amplifier are investigated in detail based on gain characteristics and numerical simulations.     

Copper-mediated oxidative tandem reactions with molecular oxygen: synthesis of 2-arylbenzoxazinone derivatives from indoles

We developed an efficient method for the transformation of indoles by utilizing a copper catalyst and molecular oxygen as the oxidant. The transformation involves a tandem oxidative process of 2-arylindoles. Our reaction afforded a variety of N-benzoyl anthranilic acids and benzoxazinones. Our investigation revealed that the choice of solvent and additives is critical in these reactions.     

Deformation of central charges,vertex operator algebras whose Griess algebras are Jordan algebras

If a vertex operator algebra $V={\oplus }_{n=0}^{\infty }{V}_n$ satisfies $\dim V_0=1$, $V_1=0$, then $V_2$ has a commutative (nonassociative) algebra structure called Griess algebra. One of the typical examples of commutative (nonassociative) algebras is a Jordan algebra. For example, the set ${\mathrm{Sym}}_d(\mathbb{C})$ of symmetric matrices of degree d becomes a Jordan algebra. On the other hand, in the theory of vertex operator algebras, central charges influence the properties of vertex operator algebras. In this paper, we construct vertex operator algebras with central charge c and its Griess algebra is isomorphic to ${\mathrm{Sym}}_d(\mathbb{C})$ for any complex number c and a positive integer d.     

Gold-black micropillar electrodes for microfluidic ELISA of bone metabolic markers

Modification with gold black considerably increased the detection current of protruding micropillar electrodes in microfluidic electrochemical enzyme-linked immunosorbent assay (ELISA).     

Arylmagnesiation of alkynes catalyzed cooperatively by iron and copper complexes

Iron and copper complexes cooperatively catalyzed the arylmagnesiation of unfunctionalized alkynes including dialkylacetylenes, where the presence of both iron and copper catalysts is essential for high yields of 2-aryl-1-alkenylmagnesium bromides.     

Asymmetric benzoin condensation promoted by chiral triazolium precatalyst bearing a pyridine moiety

Chiral triazolium salts bearing a pyridine ring were developed as N-heterocyclic carbene precursors. In the presence of the chiral triazolium salt and a base, the catalytic asymmetric benzoin condensation proceeded to afford the product in high level of chemical yield and enantioselectivity. A wide range of aromatic aldehydes were applicable to this reaction.     

One-pot synthesis of benzo[f]indole-4,9-diones from 1,4-naphthoquinones and terminal acetylenes

In this paper, a concise one-pot method for the construction of benzo[f]indole-4,9-dione motifs is described. These transformations proceed via a sequential palladium- and copper-catalyzed coupling reaction of 1,4-naphthoquinones with terminal acetylenes, followed by a copper-catalyzed intramolecular cyclization reaction of the resulting coupling product.