Synthesis of a novel series of 3-substituted [1]benzothieno[3,2-d]pyrimidine derivatives

A series of 3-substituted [1]benzothieno[3,2-d]pyrimidine derivatives has been synthesized as possible antileukemic agents by condensation of methyl 3-(ethoxymethylene)amino-2-benzothiophene carboxylate (II) with a variety of amines to afford the corresponding 3-aryl and 3-alkyl [I]benzothieno[3,2-d]pyrimidin-4(3H)-ones, Ill and IV, respectively. In addition, Mannich reactions of [I]benzothieno[3,2-d]pyrimidin-4(3H)-one (VIII) with formaldehyde and secondary amines gave the expected derivatives, IX. 3-Amino[I]benzothieno[3,2-d]-pyrimidin-4(3H)-one (VI) reacted with substituted aromatic aldehydes in the presence of boron trifluoride to yield the corresponding imines VII.     

The temperature-composition phase diagram of the HgTe?HgI2 pseudobinary system on the HgTe rich side

The temperature-composition phase diagram of the HgTe? HgI₂ system was determined from 0 to 45 Mol-% HgI₂ between 25 and 670°C using Debye-Scherrer powder X-ray diffraction techniques and differential thermal analysis. Solid solutions of HgTe and HgI₂ with the cubic, zinc blende-type structure exist above 300°C, having a maximum solubility of 11.7 ± 0.8 Mol-% HgI₂ in HgTe at 501 ± 5°C. The known monoclinic compound Hg₃Te₂I₂ is formed by a peritectic reaction upon cooling at 501 ± 5°C, with the peritectic point at approximately 37 ± 4 Mol-% HgI₂.     

Evaluation of the VIDAS Listeria (LIS) immunoassay for the detection of Listeria in foods using demi-Fraser and Fraser enrichment broths, as modification of AOAC Official Method 999.06 (AOAC Official Method 2004.06)

A multilaboratory study was conducted to compare the VIDAS LIS immunoassay with the standard cultural methods for the detection of Listeria in foods using an enrichment modification of AOAC Official Method 999.06. The modified enrichment protocol was implemented to harmonize the VIDAS LIS assay with the VIDAS LMO2 assay. Five food types--brie cheese, vanilla ice cream, frozen green beans, frozen raw tilapia fish, and cooked roast beef--at 3 inoculation levels, were analyzed by each method. A total of 15 laboratories representing government and industry participated. In this study, 1206 test portions were tested, of which 1170 were used in the statistical analysis. There were 433 positive by the VIDAS LIS assay and 396 positive by the standard culture methods. A Chi-square analysis of each of the 5 food types, at the 3 inoculation levels tested, was performed. The resulting average Chi square analysis, 0.42, indicated that, overall, there are no statistical differences between the VIDAS LIS assay and the standard methods at the 5% level of significance.     

An Efficient Approach to Spirosesquiterrenes. Synthesis of (±)β-Vetivone.

(±)β-Vetivone and (±) 10-epi-β-vetivone have been synthesized in 6 steps via an efficient spiroannelation-functionalization sequence.     

Monitoring chemotherapeutic response in RIF-1 tumors by single-quantum and triple-quantum-filtered (23)Na MRI, (1)H diffusion-weighted MRI and PET imaging

The effects of 5-fluorouracil (5FU, 150 mg/kg, ip) on subcutaneously implanted radiation-induced fibrosarcoma (RIF-1) tumors were monitored by in vivo (1)H MRI to evaluate the water apparent diffusion coefficient (ADC), by single-quantum (SQ) and triple-quantum-filtered (TQF) (23)Na MRI to evaluate compartmental Na(+) content and by positron emission tomography (PET) to evaluate 2-[(18)F]fluoro-2-deoxy-d-glucose (FDG) uptake in the tumor. The MRI experiments were performed on untreated control and treated mice once before and then daily for 3 days after treatment. The PET experiments were performed on separate groups of age- and tumor-volume-matched animals once before and then 3 days after treatment. Tumor volumes significantly decreased in treated animals 2 and 3 days posttreatment. At the same time points, in vivo MRI measurements showed an increase in both total tissue SQ (23)Na signal intensity (SI) and water ADC in treated tumors while control tumors showed no change in these parameters. TQF (23)Na SI and FDG uptake were significantly lower in treated tumors compared with control tumors 3 days after 5FU treatment. The correlated increases in total tissue (23)Na SI and water ADC following chemotherapy reflect an increase in extracellular space, while the lower TQF (23)Na SI and FDG uptake in treated tumors compared with control tumors suggest a shift in tumor metabolism from glycolysis to oxidation and/or a decrease in cell density.     

Hiding in plain sight: criminal network analysis

The United States is faced with an increasingly complex criminal enterprise. Advances in technology, communications, transport, and economies enable a highly adaptive criminal element to hide in plain site. These advances provide criminal organizations with the same global boundaries and opportunities as legitimate organizations.     

Imaging using air-coupled polymer-membrane capacitive ultrasonic arrays

Polymer-membrane capacitive ultrasonic linear and 2-D arrays have been fabricated for use in air-coupled imaging. By using arrays as receivers, there is a possibility of much faster imaging as the need for physically moving the receiver to scan a sample can be replaced by electronic multiplexing. In order to utilise this, a through-thickness air-coupled image of a composite plate has been made using a 2-D array as a receiver and a comparatively large planar source in air. This was made possible by the use of a chirp drive signal and cross-correlation on the measured waveform. Larger 2-D arrays with an increased number of elements have been simulated using a small scanned single receiver, and excellent imaging potential demonstrated. In addition two array receivers have been used in conjunction with two methods of post-processing, SAFT and ellipse crossing, to locate objects accurately.     

Discovery of a potent,selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy

Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that downregulates the insulin receptor. Inhibition of PTP1B is expected to improve insulin action, and the design of small molecule PTP1B inhibitors to treat type II diabetes has received considerable attention. In this work, NMR-based screening identified a nonselective competitive inhibitor of PTP1B. A second site ligand was also identified by NMR-based screening and then linked to the catalytic site ligand by rational design. X-ray data confirmed that the inhibitor bound with the catalytic site in the native, "open" conformation. The final compound displayed excellent potency and good selectivity over many other phosphatases. The modular approach to drug design described in this work should be applicable for the design of potent and selective inhibitors of other therapeutically relevant protein tyrosine phosphatases.     

Study of the Log-Layer Structure in Wall Turbulence Over a Very Large Range of Reynolds Number

Studies of the logarithmic layer structure in turbulent boundary layers are presented that span three orders of magnitude change in Reynolds number. The experiments considered used two separate laboratory scale facilities, as well as the atmospheric surface layer at the SLTEST facility in Utah. Several experimental techniques were used in order to probe the three-dimensional nature of the flow structures. The main focus is on two-point correlation statistics at a given z/δ, which are found to agree well over all Reynolds numbers when scaled with an outer length-scale. Large-scale coherence recently noted in the logarithmic region of laboratory-scale boundary layers is also found to be present in the atmospheric surface layer flow. Recent findings regarding the influence of these large scale motions on the near-wall region are also presented.     

The Equilibrium Partial Pressure of HgI2 over and Thermodynamic Properties of Hg3Te2I2 1)

The high temperature vaporization pattern of Hg₃Te₂I₂(s,l) shows four distinctly different regimes, similar to those of the HgTe vaporization. The most predominant species in the vapor phase in all four regimes is HgI₂(g), followed by Hg(g) and, possibly, Te₂I₂(g). The width of the “homogeneity range” of Hg₃Te₂I₂(s) was determined to be less than about 0.17 mole‐% HgI₂. Applying the second‐law method to the vaporization of HgTe‐saturated Hg₃Te₂I₂(s) at higher temperatures yields the heat and entropy of vaporization of 20.9 ± 2.3 (kcal/mole) and of 27.5 ± 2.8 (cal/mole K), respectively, with estimated total uncertainties of less than ± 5.8 (kcal/mole) and ± 7.6 (cal/mole K), at an average temperature of 722 K. With an estimated heat capacity function of Hg₃Te₂I₂(s) and estimated thermodynamic values for HgI₂‐saturated HgTe(s), the heat of formation and absolute entropy of Hg₃Te₂I₂(s) are computed to be = ?49.7 ± 1.1 (kcal/mole) and = 97.3 ± 1.4 (cal/mole K), with estimated total uncertainties of ± 8.3 (kcal/mole) and ± 14.0 (cal/mole K). The combined results of this investigation provide valuable information for the crystal growth of this material from the vapor and molten phase.