gebhart/patrepeval huggingface dataset:
WB 4101-Related Compounds. 2. Role of the Ethylene Chain Separating Amine and Phenoxy Units on the Affinity for α1-Adrenoreceptor Subtypes and 5-HT1A Receptors (1999)

WB 4101 (1)-related benzodioxanes were synthesized by replacing the ethylene chain separating the amine and the phenoxy units of 1 with a cyclopentanol moiety, a feature of 6, 7-dihydro-5-[[(cis-2-hydroxy-trans-3-phenoxycyclopentyl)amino]meth yl] -2-methylbenzo[b]thiophen-4(5H)-one that was reported to display an intriguing selectivity profile at alpha(1)-adrenoreceptors. This synthesis strategy led to 4 out of 16 possible stereoisomers, which were isolated in the case of (-)-3, (+)-3, (-)-4, and (+)-4 and whose absolute configuration was assigned using a chiral building block for the synthesis of (-)-3 starting from (+)-(2R)-2, 3-dihydro-1,4-benzodioxine-2-carboxylic acid ((+)-9) and (1S,2S, 5S)-2-amino-5-phenoxycyclopentan-1-ol ((+)-10). The aim of this project was to further investigate whether it is possible to differentiate between these compounds with respect to their affinity for alpha(1)-adrenoreceptor subtypes and the affinity for 5-HT(1A) receptors, as 1 binds with high affinity at both receptor systems. The biological profiles of reported compounds at alpha(1)-adrenoreceptor subtypes were assessed by functional experiments in isolated rat vas deferens (alpha(1A)), spleen (alpha(1B)), and aorta (alpha(1D)) and by binding assays in CHO and HeLa cells membranes expressing the human cloned alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors, respectively. Furthermore, the functional activity of (-)-3, (+)-3, (-)-4, and (+)-4 toward 5-HT(1A) receptors was evaluated by determining the induced stimulation of [(35)S]GTPgammaS binding in cell membranes from HeLa cells transfected with human cloned 5-HT(1A) receptors. The configuration of the cyclopentane unit determined the affinity profile: a 1R configuration, as in (+)-3 and (-)-4, conferred higher affinity at alpha(1)-adrenoreceptors, whereas a 1S configuration, as in (-)-3 and (+)-4, produced higher affinity for 5-HT(1A) receptors. For the enantiomers (+)-4 and (-)-4 also a remarkable selectivity was achieved. Functionally, the stereoisomers displayed a similar alpha(1)-selectivity profile, that is alpha(1D) > alpha(1B) > alpha(1A), which is different from that exhibited by the reference compound 1. The epimers (-)-3 and (+)-4 proved to be agonists at the 5-HT(1A) receptors, with a potency comparable to that of 5-hydroxytryptamine.
Microbially Safe Utilization of Non-Inactivated Oats (Avena sativa L.) for Production of Conjugated Linoleic Acid (2006)

A microbially safe process for the enrichment of conjugated linoleic acid (CLA) in oats was developed. The process consists of hydrolysis of oat lipids by non-inactivated oat flour, followed by propionibacterium-catalyzed isomerization of the resulting free linoleic acid to CLA. The first stage was performed at water activity (a(w)) 0.7, where hydrolysis of triacylglycerols progressed efficiently without growth of the indigenous microflora of flour. Thereafter, the flour was incubated as a 5% (w/v) aqueous, sterilized slurry with Propionibacterium freudenreichii ssp. shermanii. The amount of CLA produced in 20 h was 11.5 mg/g dry matter corresponding to 116 mg/g lipids or 0.57 mg/mL slurry. The oat flour had also the capability to hydrolyze exogenous oils at a(w) 0.7. Sunflower oil, added to increase linoleic acid content in triacylglycerols 2.7-fold, was hydrolyzed rapidly. Isomerization of this oil-supplemented flour as a 5% slurry gave final CLA content of 22.3 mg/g dry matter after 50 h of fermentation, corresponding to 118 mg/g lipids or 1.14 mg/mL slurry. Storage stability of CLA in fermented oat slurries at 4 degrees C was good.
Observation of gas-liquid-solid interface using total reflection microscope with polarization plate (2016)

PVA (Polyvinyl acetal) brushes have been widely used for a wet cleaning in semiconductor device fabrication. To better understanding the lubrication condition between a PVA brush and cleaning surfaces, we observed gas-liquid-solid interface using a total reflection microscope with polarization plates. First we investigated the real contact area of a POM (Polyoxymethylene) ball by applying a normal load in air and water. Then we observed the contact condition of a PVA brush. As a result, the observed real contact areas of the POM ball were agreed with the estimation from the Hertzian contact theory. In addition, the real contact area between a PVA brush and a glass plate in water was also able to observe. The real contact areas were increased with increase the normal force acting on the PVA brush. We concluded that the part of a PVA brush is contact with a cleaning surface.
A Unified Dynamic Model for Bi-directional DC-DC Converter (2014)

This paper presents a unified model for bi-directional DC-DC converters for both directions of power flow. The bi-directional DC-DC converter is analyzed using a seamless dynamic model with an independent voltage source and an independent current source, which polarity depends on the direction of the power flow. A small signal model is derived using a state space averaging method. Furthermore, the transient response and the frequency characteristics are discussed. Example circuits for bi-directional DC-DC converter are investigated analytically, using simulation, and experimentally.
Patterns of angiogenesis in nonsmall‐cell lung carcinoma (2001)

BACKGROUND Tumor angiogenesis plays a pivotal role in tumor growth, maintenance, and metastasis. The objective of the current study was to evaluate the prognostic value of estimates of tumor angiogenesis and vascular endothelial growth factor (VEGF) status in 143 primary tumors from patients who underwent radical surgery for nonsmall-cell lung carcinoma (NSCLC). METHODS Tumor sections were stained by immunohistochemistry for CD34 and VEGF. Angiogenesis was estimated both by a modification of the method described by Weidner and by the use of a 25-point Chalkley eyepiece graticule. VEGF intensity was evaluated semiquantitatively in three groups of patients. The vascular data were correlated with histopathologic tumor type and grade, TNM classification, patient age, and the endpoint (death). RESULTS The estimates of vascular score did not reveal any prognostic information. In 35 patients (24%), invasive tumor growth was identified with a highly ordered alveolar microvessel pattern. In parallel sections, the intensity of VEGF staining was weak in tumors that exhibited an alveolar microvessel pattern only, and it was more intense in tumors that demonstrated a mixed alveolar and diffuse angiogenic pattern. The 35 patients with alveolar microvessel pattern had a significantly better survival (P = 0.007). In a Cox multivariate analysis, the results demonstrated an independent bad prognostic value of high disease stage (P < 0.0001), adenocarcinoma (P = 0.004), greater age (P = 0.01), and angiogenic microvessel pattern (P = 0.01). CONCLUSIONS The authors believe that the alveolar vascular pattern represented preexisting alveolar vessels, that is, the alveoli were filled up by tumor cells that exploited the existing highly vascular bed of the lungs. Therefore, this subgroup was characterized by tumor progression without the induction of angiogenesis. The current data do not support a significant prognostic role for tumor angiogenesis in patients who are diagnosed with NSCLC. This may have implications for therapy aimed at inhibiting tumor growth by the inhibition of angiogenesis. Cancer 2001;91:1500–9. © 2001 American Cancer Society.
Crystal structure of crystal structure of 4,5,9,10-tetrathiocino[1,2-b;5,6- b']diimidazolyl-1,3,6,8-tetramethyl-2,7-dione, C10H12N4O2S4 (2008)

Article Crystal structure of crystal structure of 4,5,9,10-tetrathiocino[1,2-b;5,6- b']diimidazolyl-1,3,6,8-tetramethyl-2,7-dione, C10H12N4O2S4 was published on September 1, 2008 in the journal Zeitschrift für Kristallographie - New Crystal Structures (volume 223, issue 3).
Phase I trial with a combination of docetaxel and 153Sm- EDTMP in patients (pts) with castration-resistant metastatic prostate cancer (mCRPC) (2009)

5155 Background: Bone targeted therapy holds great promise for improving outcomes in mCRPC. Preclinical data strongly supported biological synergism of docetaxel (Tax) and 153 Sm-EDTMP (Sm) in mCRPC. Concurrent Tax and Sm regimens were reported feasible and tolerable in phase I studies. This study was designed to evaluate toxicity and preliminary efficacy of 2 cycles (12 wks/cycle, C) of concomitant standard dose/schedule of Sm plus Q3 wks schedule of Tax in mCRPC. Methods: mCRPC pts with progressive bone metastases were treated in 4 cohorts ( CH). Previous Tax and palliative RT to bone was admissible. Dose escalation of Tax was implemented if no DLT was observed in the preceding CH. Tax doses (on days 1, 22, per 12 wk cycle) were given as follows: CH 1- 50mg/m 2 (C1 and 2); CH 2–75mg/m 2 (C1) and 50mg/m 2 (C2); CH3 - 75mg/m 2 (C1 and 2) and CH4 ( Tax day 1, 22, 43 per 12 wk C) 75mg/m 2 (C1 and 2). Sm was administered on days 2 (Q12 wks X 2) at dose of 1 mCi/kg/cycle (max. of 2 cycles). Disease status was assessed (with bone /CT scans and PSA) after every cycle. Results: Thirteen pts with progressive bone metastases were enrolled. Three had prior Tax and 3 had prior palliative radiation. Thirteen pts received total 20 cycles in 4 cohorts. Toxicity was primarily hematological. There were total 34 episodes Grade 3/4 neutropenia with a median 7 (range 7 -14) days to recovery to ≤ grade1. Tax dose was reduced to 50% in 2 CH4 pts at C2. Only 1 DLT G3 thrombocytopenia occurred on cohort 4 with duration of 9 wks. Median baseline PSA was 100.4 ng/ml (range 8.6 - 1064), 9/13 (69%) pts had PSA&gt;50% decrease. Median time to disease progression was 147 days (range 72 days - 10 months + ); 6/13 (46%) pts had stable/improved bone scans at 6 months and 8/8 (100%) symptomatic pts had improvement in pain. Conclusions: Concurrent 6-month administration of 2 and possibly 3 full dose /standard schedule of Tax with 2 full doses of Sm is feasible with reversible bone marrow suppression. The combination may provide additional clinical benefits for mCRPC pts with extensive bone metastasis. No significant financial relationships to disclose.
Selective inhibition of tropomyosin-receptor-kinase A (TrkA) reduces pain and joint damage in two rat models of inflammatory arthritis (2016)

By using two models of varying inflammation we demonstrate for the first time that selective inhibition of TrkA may reduce carrageenan-induced or CIA-induced pain behaviour in rats, in part through potentially inhibiting synovial inflammation, although direct effects on sensory nerves are also likely. Our observations suggest that inflammatory arthritis causes pain and the presence of inflammation is fundamental to the beneficial effects (reduction in pain and pathology) of NGF blockade. Further research should determine whether TrkA inhibition may ameliorate human inflammatory arthritis.
Unsupervised learning techniques for an intrusion detection system (2004)

With the continuous evolution of the types of attacks against computer networks, traditional intrusion detection systems, based on pattern matching and static signatures, are increasingly limited by their need of an up-to-date and comprehensive knowledge base. Data mining techniques have been successfully applied in host-based intrusion detection. Applying data mining techniques on raw network data, however, is made difficult by the sheer size of the input; this is usually avoided by discarding the network packet contents.In this paper, we introduce a two-tier architecture to overcome this problem: the first tier is an unsupervised clustering algorithm which reduces the network packets payload to a tractable size. The second tier is a traditional anomaly detection algorithm, whose efficiency is improved by the availability of data on the packet payload content.
Synthesis of New Cyclic andAcyclic 5-Halouridine Derivatives as Potential Antiviral Agents (2009)

The synthesis of new cyclic and acyclic nucleoside analogues was achieved by alkylation of 5-halogenated 6-(2,4-dichlorophenoxymethyl)pyrimidine-2,4-dione following the Vorbrüggen coupling procedure. Nucleoside analogues of the 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)-type were obtained as well as analogues of ganciclovir, acyclovir, and ribonucleosides. All compounds were tested against a variety of viruses. Three of the new compounds were potent and selective anti-HIV-1 inhibitors.
On the Effective Turn-Off of GTO by a Small Saturable Core (1987)

A new turn-off circuit for gate-turn-off (GTO), which is simple and of low energy consumption is presented. The principle is based on the resonance between saturating inductance of the magnetic core and the parasitic capacitance included in GTO. Analytical as well as experimental results are presented.
Medicinal Chemistry of Alicyclic β‐Amino Acids (2011)

Compared with their open-chain congeners, alicyclic β-amino acids are less prominent in the literature. However, over recent years the interest in alicyclic β-amino acids has steadily increased, and these have become an intriguing topic in synthetic and medicinal chemistry. In detail, alicyclic β-amino acids frequently occur in pharmacologically important compounds and additionally serve as important structure-forming elements in β-peptides. Herein, we give a comprehensive review of the synthesis and pharmacological profile of five- and six-membered alicyclic β-amino acids with an impact on medicinal chemistry. Important alicyclic β-amino acids such as cispentacin, icofungipen, and tilidine are discussed.
Partitioning of Rb and Sr between haplogranitic melts and aqueous fluids (2008)

Author: Borchert, M. et al.; Genre: Journal Article; Finally published : 2008; Keywords: Abstracts of the 18th Annual V.M. Goldschmidt Conference; Title: Partitioning of Rb and Sr between haplogranitic melts and aqueous fluids
Elf-1 Regulates Basal Expression from the T Cell Antigen Receptor ζ-Chain Gene Promoter (1998)

Abstract In mature T cells, limited synthesis of the TCR-ζ subunit is primarily responsible for regulating surface expression of TCRs. Transcription of ζ is directed by a complex promoter that includes two potential binding sites for the Ets family of transcription factors at −52 (zEBS1) and −135 (zEBS2). Mutation of these two sites results in a marked reduction of transcription from this promoter. Using electrophoretic mobility shift analysis, Elf-1 was demonstrated to be the Ets family member that binds to these sites. One site, zEBS1, matches the optimal Elf-1 consensus sequence in eight of nine bases, making it the best match of any known mammalian Elf-1 binding site. A role for Elf-1 in TCR-ζ trans-activation was confirmed by ectopic expression of Elf-1 in COS-7 cells. This resulted in an increase in TCR-ζ promoter activity that mapped to zEBS1 and zEBS2. Additional support for the involvement of Elf-1 in TCR-ζ trans-activation derives from the finding that a GAL4-Elf-1 fusion protein trans-activated TCR-ζ promoter constructs that had been modified to contain GAL4 DNA binding sites. These results demonstrate that Elf-1 plays an essential role in the trans-activation of a constitutively expressed T cell-specific gene, and that trans-activation occurs in the context of the native promoter in both lymphoid and nonlymphoid cells. Taken together with the existing literature, these data also suggest that the requirement for inducible factors in Elf-1-mediated trans-activation may decrease as the affinity and number of Elf-1 sites increase.
The movement of pyruvate, lactate and lactate dehydrogenase into rabbit oviductal fluid (1979)

Pyruvate, lactate and lactate dehydrogenase appeared linearly in 2 ml 0.9% NaCl recirculated through the rabbit oviduct for 4 h in vivo. In oviducts from rabbits injected 3 days previously with 100 i.u. hCG, the rate of appearance of all three constituents was considerably reduced. It is considered unlikely that the lactate dehydrogenase secreted brings about the interconversion of pyruvate and lactate in the oviduct lumen.
Influence of cation size on the thermoelectric behavior of salt-doped organic nanocomposite thin films (2021)

Developing and understanding novel doping strategies for thermoelectric materials is imperative to efficiently convert waste into a useful voltage. One such method for improving the power factor of polymer nanocomposites is through salt doping. The cation size of a monovalent salt dopant was varied in a layer-by-layer (LbL)-assembled film composed of poly(diallyldimethylammonium chloride) (PDDA) and double-walled carbon nanotubes (DWNTs) stabilized by poly(3,4-ethylenedioxythiophene):poly(styrene sulfonate) [PEDOT:PSS]. Doping a 20 bilayer PDDA/DWNT-PEDOT:PSS film doped with 3 mmol CsCl yields the maximum power factor of 485 ± 29 μW m−1 K−2. This value was obtained through a five times increase in the electrical conductivity with a minimal decrease in the Seebeck coefficient relative to the undoped film. Cs+ is believed to more heavily dope the carbon nanotube network due to its relatively larger hydrophobicity, while also separating PEDOT from PSS due to charge screening. This study demonstrates the significance of the salt dopant identity, and the insight herein can likely be applied more broadly to improve a variety of organic thermoelectric materials.
Maximum Likelihood Surface Profilometry Via Optical coherence Tomography (2022)

Optical coherence tomography (OCT) using Fourier domain processing can resolve micrometer-scale depth information. However, the conventional volumetric reconstruction approach is unnecessary for opaque samples with only one reflector per lateral position, and the required sample interpolation degrades performance. In this paper, we show that surface depth profilometery with a Fourier-domain OCT system simplifies to a sinusoidal parameter estimation problem. We derive approximate maximum likelihood estimators for the sample depth and reflectivity, which can easily be computed by backprojecting the data without interpolating. Iterative refinement further improves results at high signal-to-noise ratio (SNR). We demonstrate the performance of the technique compared to the conventional Fourier transform approach on both simulated and experimental data collected with a spectral-domain OCT system. Our results show that maximum likelihood profilometry is fast and more robust to noise than the Fourier approaches at moderate SNR.
ChemInform Abstract: Ab initio Theoretical Predictions of C28, C28H4, C28F4, (Ti C28)H4, and M C28 (M: Mg, Al, Si, S, Ca, Sc, Ti, Ge, Zr, and Sn). (1993)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Möglichkeiten zur Darstellung des supraorbitalen Gefäßplexus für die präoperative Lappenplanung bei größeren Nasenrekonstruktionen (2023)

Einleitung Zur plastischen Rekonstruktion komplexer Nasendefekte wird oft der axial gestielte paramediane Stirnlappen eingesetzt. Die Blutversorgung erfolgt primär über die A. supratrochlearis, die zum supraorbitalen Gefäßplexus gehört. Fragestellung: Das Ziel der prospektiven Anwendungsstudie ist zu beurteilen, inwieweit eine Perfusionsanalyse des supraorbitalen Gefäßplexus durch eine dynamische 4D-CT Bildgebung für die präoperative Planung des Lappendesigns möglich ist.
Enantioselective Synthesis of β‐Amino Acid Derivatives Enabled by Ligand‐Controlled Reversal of Hydrocupration Regiochemistry (2020)

A Cu-catalyzed enantioselective hydroamination of α,β-unsaturated carbonyl compounds for the synthesis of β-amino acid derivatives was achieved through ligand-controlled reversal of the hydrocupration regioselectivity. While the hydrocupration of α,β-unsaturated carbonyl compounds to form α-cuprated species has been extensively investigated, we report herein that, in the presence of an appropriate ancillary chiral ligand, the opposite regiochemistry can be observed for cinnamic acid derivatives, leading to the delivery of the copper to the β-position. This copper can react with an electrophilic aminating reagent, 1,2-benzisoxazole, to provide enantioenriched β-amino acid derivatives, which are important building blocks for the synthesis of natural products and bioactive small molecules.
Groundwater Level Trends and Drivers in Two Northern New England Glacial Aquifers (2016)

Abstract We evaluated long‐term trends and predictors of groundwater levels by month from two well‐studied northern New England forested headwater glacial aquifers: Sleepers River, Vermont, 44 wells, 1992‐2013; and Hubbard Brook, New Hampshire , 15 wells, 1979‐2004. Based on Kendall Tau tests with Sen slope determination, a surprising number of well‐month combinations had negative trends (decreasing water levels) over the respective periods. Sleepers River had slightly more positive than negative trends overall, but among the significant trends ( p &lt; 0.1), negative trends dominated 67 to 40. At Hubbard Brook, negative trends outnumbered positive trends by a nearly 2:1 margin and all seven of the significant trends were negative. The negative trends occurred despite generally increasing trends in monthly and annual precipitation. This counterintuitive pattern may be a result of increased precipitation intensity causing higher runoff at the expense of recharge, such that evapotranspiration demand draws down groundwater storage. We evaluated predictors of month‐end water levels by multiple regression of 18 variables related to climate, streamflow, snowpack, and prior month water level. Monthly flow and prior month water level were the two strongest predictors for most months at both sites. The predictive power and ready availability of streamflow data can be exploited as a proxy to extend limited groundwater level records over longer time periods.
Refraction measurements with an open-view binocular Shack-Hartmann wavefront sensor (2010)

We have developed an open-view binocular Shack Hartmann wavefront sensor to measure accommodation, vergence, pupil size, and monochromatic aberrations of both eyes. Two optical channels, comprised of Shack-Hartmann wavefront sensors and anterior imaging cameras, were laterally aligned to both eyes. A dichroic mirror reflected near infrared light between the eye and the measuring instrument while visible light from an object passed thorough the mirror to the eye. We used one million pixel CCD cameras and three fast PCs to grab images from the sensors and analyze data. We confirmed the accuracy and precision of the refraction using model eyes and human eyes. We measured refraction of 50 eyes in 25 normal subjects using the wavefront sensor and a commercial autorefractometer. Accuracy of refraction was found to be 0.03 diopters when we measured the model eyes. The precision was less than 0.18 diopters for human eyes. Correlation coefficients of determination between the wavefront sensor and commercial autorefractometer were 0.96 for both eyes. We believe the open-view-binocular wavefront sensor will be a useful instrument for the investigation of the refraction and accommodation under natural viewing condition.
A multi-layered head phantom for microwave investigations of brain hemorrhages (2016)

A head phantom for microwave investigations is developed. It consists of a skull bone with realistic dielectric properties of cancellous and cortical bone. The skull phantom is filled with liquids and semi-solids that dielectrically represent the white/gray matter and blood, respectively.