Discovery of N-(3-{4-[(3-fluorobenzyl)oxy]phenoxy}propyl)-2-pyridin-4-ylacetamide as a potent and selective reverse NCX inhibitor

In the setting of heart failure and myocardial ischemia-reperfusion, the sodium-calcium exchanger (NCX) can lead to calcium overload, which is responsible for contractile dysfunction and arrhythmia. NCX is an attractive target for treatment in heart failure and myocardial ischemia-reperfusion. We have designed and synthesized a series of benzyloxyphenyl derivatives based on compound 3. These derivatives have been evaluated for their inhibitory activity against both the reverse and forward modes of NCX. We have discovered a novel potent and selective reverse NCX inhibitor (12) with an IC50 value of 0.085 microM against reverse NCX.     

Photocatalytic decomposition of liquid water on a NiOSrTiO3 catalyst

The photocatalytic decomposition of liquid water on a NiOSrTiO₃ catalyst was studied. The activity was increased considerably by an improvement of pretreatment conditions and using concentrated NaOH solution.     

Development of a curie-point headspace sampler for capillary gas chromatography

A Curie-point headspace sampler (CPHS) equipped with a purge and trap sampler has been developed for use with capillary gas chromatography. The new system can handle a variety of samples, including gases, liquids, and solids, and can also be used as a pyrolyzer.     

The fixed boundary value problems for the equations of ideal Magneto-Hydrodynamics with a perfectly conducting wall condition

The equations of ideal Magneto-Hydrodynamics are investigated concerning initial boundary value problems with a perfectly conducting wall condition. The local in time solution is proved to exist uniquely, provided that the normal component of the initial magnetic field vanishes everywhere or nowhere on the boundary.     

Structures, biological activities, and total syntheses of 13-hydroxy- and 13-acetoxy-14-nordehydrocacalohastine, novel modified furanoeremophilane-type sesquiterpenes from Trichilia cuneata

[reaction: see text] 13-Hydroxy-14-nordehydrocacalohastine (2) and 13-acetoxy-14-nordehydrocacalohastine (3), two novel modified furanoeremophilane-type sesquiterpenes isolated from Trichilia cuneata, showed inhibitory activities for membrane lipid peroxidation in mitochondria and microsomes. The first, highly convergent total syntheses of new compounds 2 and 3 have also been achieved via a palladium-mediated three-component coupling reaction between 2-iodotoluene (7), 1-penten-4-yn-3-ol (8), and diethyl ethoxymethylenemalonate (9).     

Synthesis of unnatural 1-methyl-2-quinolone derivatives

Unnatural 1-methyl-2-quinolone derivatives were synthesized by regioselective C-C bond formation. When 1-methyl-3,6,8-trinitro-2-quinolone (TNQ) was treated with enamines, nucleophilic addition readily occurred at the 4-position, and succeeding hydrolysis of enamine moiety followed by elimination of nitrous acid furnished 4-acylmethyl-1-methyl-6,8-dinitro-2-quinolones. The same products could be prepared by the reaction of TNQ with ketones in the presence of triethylamine. The present reaction enabled the introduction of various kinds of acylmethyl groups substituted with alkyl, aryl or hetaryl groups.     

Study of Serrated Aperture for a Cassegrain Booster Amplifier

The upgrade of the actual large laser facilities (GEKKO XII in our case) implies an increase of filling-factor, but avoiding the generation of spatial high frequencies. To reach that purpose we intend to construct the beams using serrated apertures with an optimised shape. The performances of our system led after simulation to a 70% filling factor with less than 2% fluctuation on the laser pattern intensity map. The optimisation was also checked from a financial point of view. The usual serrated apertures are already giving good results, so we attached ourselves to seek for financial efficiency.