One-step synthesis of differently bis-functionalized isoxazoles by cycloaddition of carbamoylnitrile oxide with β-keto esters

A new protocol for synthesizing different functionalized isoxazoles is provided. Carbamoylnitrile oxide generated from nitroisoxazolone underwent inverse electron-demand 1,3-dipolar cycloaddition with 1,3-dicarbonyl compounds in the presence of magnesium acetate that formed magnesium enolatein situ. Although electron-deficient trifluoroacetoacetate did not undergo this cycloaddition under the same conditions, conversion to sodium enolate furnish the corresponding bis-functionalized trifluoromethylisoxazole. The DFT calculations using B3LYP 6-31G+(d,p) also supported the aforementioned reactivity

DsTau: Study of tau neutrino production with 400 GeV protons from the CERN-SPS

In the DsTau experiment at the CERN SPS, an independent and direct way to measure tau neutrino production following high energy proton interactions was proposed. As the main source of tau neutrinos is a decay of Ds mesons, produced in proton-nucleus interactions, the project aims at measuring a differential cross section of this reaction. The experimental method is based on a use of high resolution emulsion detectors for effective registration of events with short lived particle decays. Here we present the motivation of the study, details of the experimental technique, and the first results of the analysis of the data collected during test runs, which prove feasibility of the full scale study of the process in future

DHMEQ, a novel NF-kappaB inhibitor, suppresses growth and type I collagen accumulation in keloid fibroblasts

Background:Keloid is a benign dermal tumor characterized by proliferation of dermal fibroblasts and overproduction of extracellular matrix (ECM). Nuclear factor kappaB (NF-κB) plays an important role in regulation of inflammation, immune response and cell proliferation. Activation of the NF-κB pathway is thought to be closely linked to abnormal cell proliferation and ECM production in keloid fibroblasts. Objective:This study was set out to investigate the effects of a novel selective NF-κB inhibitor, dehydroxymethylepoxyquinomicin (DHMEQ), on keloid fibroblasts. Methods:Primary normal and keloid dermal fibroblasts were used for this study. NF-κB activity was assessed by DNA-binding assay and immunohistochemistry. The effect of DHMEQ was evaluated by cell viability, cell growth and type I collagen accumulation. Results:Basal NF-κB activity was constitutively elevated in keloid fibroblasts, indicating that this pathway is involved in keloid pathogenesis. DHMEQ markedly reduced cell proliferation and type I collagen accumulation in keloid fibroblasts. Conclusion:The inhibition of NF-κB by DHMEQ may be an attractive therapeutic approach for keloids

Effect of transcriptional regulatory sequences on autonomous replication of plasmids in transient mammalian systems.

Transcriptional regulatory sequences often influence the efficiency of DNA replication, directly or indirectly, in bacteria, yeast, and animal virus systems. We have tested several transcriptional regulatory sequences for affecting DNA replication, based on pUC vector, in transient systems. Autonomous replication of transfected plasmids was assayed by PCR amplification of the fragments derived from the plasmids, which had replicated in mammalian cells. By this highly efficient method of detecting replicated molecules, pUC19, but not pUC18, showed a week replication activity in transfected cells. Nucleotide sequences around the HindIII site in pUC19 were required for replication. Monomers or dimers of the octamer transcription motif of the mouse immunoglobulin heavy chain gene, inserted in multicloning sites of pUC19, could stimulate replication, while the 4- or 6-mers did not, in contrast to the results on its transcription activity. Other transcriptional elements including AP1, HSE, and E2F also stimulated replication, but neither CRE nor Sp1 binding motif did. These results suggest that at least some of the transcriptional regulatory sequences function as-modulators of DNA replication as well as of transcription

Estimation of passenger car CO2 emissions by population density class based on Japanese vehicle inspection certificate data

Estimates of passenger car CO2 emissions that reflect regional characteristics are useful for predicting the effects of electrification, modal shifts in transport, and urban compactness. To date, differences in emissions have often been estimated based on the regional differences in the number of vehicles owned. Regional differences in mileage were estimated from the counts of the Origin and Destination Surveys in the Road Traffic Census. In this study, by utilizing the mileage data from the vehicle inspection certificate data, it was possible to reflect the differences in mileage per vehicle in detailed regional terms. The higher the population density, the smaller was the mileage per vehicle. Based on this, we calculated the CO2 emissions from passenger cars by municipality nationwide and estimated the CO2 emissions and population share by grid population density. In areas of 3000–10,000 persons/km2, which accounts for approximately 40% of Japan's population, emissions per person approximated the national average. However, in areas with 1000–3000 persons/km2 (approximately 20% of the population), emissions per person were approximately 30% higher; while with 100–1000 persons/km2 (approximately 1.5% of the population), they were approximately 70% higher; and with 10,000 persons/km2 (approximately 25% of the population), they were approximately 70% lower. A map was produced for use when considering the cities and regions suitable for a decarbonized society as well as policies such as electrification, modal shift, and coordination of urban centers

Nucleophilic B-amination of pyridine nuclei

—3-Bromo-4-nitropyridine N-oxide behaves as a useful substrate for causing nucleophilic substitution at the -position (3-position) with amines to afford 3-aminopyridine derivatives