gebhart/patrepeval huggingface dataset:
Enhanced D1 Affinity in a Series of Piperazine Ring Substituted 1-Piperazino-3-Arylindans with Potential Atypical Antipsychotic Activity (1995)

A study of the effect of aromatic substitution on D1 and D2 affinity in a series of previously reported trans-1-piperazino-3-phenylindans shows similar structure-activity relationships for the two receptor sites. 6-Substituted derivatives have affinity for both receptors, and 6-chloro-or 6-fluoro-substituted derivatives show preference for D1 receptors. D1 affinity and selectivity are significantly increased in a series of new piperazine ring substituted derivatives. Potent D1 and D2 antagonism in vivo are confined to derivatives with relatively small substituents in the 2-position of the piperazine ring (e.g. 2-methyl,2,2-dimethyl, 2-spirocyclobutyl or 2-spirocyclopentyl). Consequently, the effect of aromatic substitution is examined in a series of 1-(2,2-dimethylpiperazino)-3-arylindans. All these compounds except the 4-, 5-, 7- and 4'-chloro-substituted derivatives have potent D1 affinity (IC50's below 10 nM) and the majority of the compounds antagonize SK&F 38393-induced circling in 6-OHDA-lesioned rats with ED50 values about 1 mumol/kg. In vitro all compounds show preference for D1 receptors, but in vivo they are equally effective as D1 and D2 antagonists. The compounds have high affinity for 5-HT2 receptors and selected compounds show high affinity for alpha 1 adrenoceptors. Furthermore, a subgroup consisting of (-)-38, (-)-39, (-)-41, and (-)-54 does not induce catalepsy in rats. These compounds have the potential of being "atypical" antipsychotics and have consequently been selected for further studies. The non-receptor-blocking enantiomers are shown to be inhibitors of DA and NE uptake in accordance with previous observations in compounds unsubstituted in the piperazine ring. Two compounds, (+)-38 and (+)-40, block DA uptake with IC50 values below 10 nM. Finally, the observed structure-activity relationships are discussed in relation to previously published pharmacophore models for D2 and 5-HT2 receptors. It is concluded that the piperazine substituents might induce a different binding mode at the dopamine receptor sites, perhaps only at the D1 receptor site.
PALLADIUM(II) CATALYZED SYNTHESIS OF ARYL CYANIDES FROM ARYL HALIDES (1973)

Abstract In the presence of Pd(II) salts, substitution reaction of aryl halides with potassium cyanide occurs readily which affords a simple and beneficial method for aryl cyanide synthesis.
Chemical and Pharmacological Research on Plants from the Genus <i>Senecio</i> (2011)

by Yan Yanga)b), Lei Zhaoa)b), Yu-Fang Wanga), Man-Li Changa), Chang-Hong Huoa), Yu-Cheng Gua)c), Qing-Wen Shi*a), and Hiromasa Kiyota*d) a) Department of Medicinal Natural Product Chemistry, School of Pharmaceutical Sciences, Hebei Medical University, Shijiazhuang 050017, P. R. China (phone: þ86-311-86265634; e-mail: shiqingwen@hebmu.edu.cn) b) The Tumor Hospital of Yunnan Province, the Third Affiliated Hospital of Kunming Medical University, 519 Kunzhou Road, Kunming 650118, P. R. China c) Jealott s Hill International Research Centre, Syngenta, Berkshire, RG426EY, UK d) Laboratory of Applied Bioorganic Chemistry, Division of Life Science, Graduate School of Agricultural Sciences, TohokuUniversity, 1-1 Tsutsumidori-Amamiya, Aoba-ku, Sendai, 981-8555, Japan (phone/fax: þ81-22-7178785; e-mail: kiyota@biochem.tohoku.ac.jp)
A review of experimental evidence for the carcinogenicity of man-made vitreous fibers. (1986)

This paper reviews experimental studies on the carcinogenicity of man-made vitreous fibers. Long-term inhalation studies using several animal species and dust preparations of fibrous glass, rock wool or slag wool have produced little evidence of pulmonary fibrosis or pulmonary tumors. While some intratracheal injection studies found almost no pathological changes in lung tissue, some showed that pulmonary fibrosis can occur. Only one intratracheal injection study has reported that vitreous fibers can be carcinogenic; in contrast, many workers have reported that, following intrapleural or intraperitoneal injection, man-made vitreous fibers are highly carcinogenic, and tumor production appears to be closely related to fiber size. In vitro tests confirm that vitreous fibers can be toxic and can cause neoplastic transformation of cultured cells. The discrepancies between some experimental studies probably result from the relatively high solubility of most vitreous fibers. It seems likely that, while these fibers can survive in body cavities long enough to cause tumor production, they dissolve in lung tissue fast enough to have relatively little harmful effect. Rock-wool fibers appear more durable than glass- or slag-wool fibers, and, with similar fiber numbers and sizes in any dust cloud, this material is the most likely to have harmful potential.
Emergency Vehicle Detection on Heavy Traffic Road from CCTV Footage Using Deep Convolutional Neural Network (2019)

A highly populated country like Bangladesh faces too much traffic jam. Sometimes emergency vehicles like ambulance, fire-fighter get stuck in the traffic causing threat to life in many cases. It is important to give priority to this car and help to clear its path. But it is difficult or sometimes impossible for traffic police to handle this. For this reason, we need an automated system that will be able to detect an emergency car in heavy traffic road, let the controller know or automatically navigate other cars to clear its path. In this work, we have proposed an automated system to detect emergency cars from CCTV footage using the deep convolutional neural network. Our method has shown good result in detecting and classifying emergency cars.
Enhanced Catalysis from Multienzyme Cascades Assembled on a DNA Origami Triangle (2019)

Developing reliable methods of constructing cell-free multienzyme biocatalytic systems is a milestone goal of synthetic biology. It would enable overcoming the limitations of current cell-based systems, which suffer from the presence of competing pathways, toxicity, and inefficient access to extracellular reactants and removal of products. DNA nanostructures have been suggested as ideal scaffolds for assembling sequential enzymatic cascades in close enough proximity to potentially allow for exploiting of channeling effects; however, initial demonstrations have provided somewhat contradictory results toward confirming this phenomenon. In this work, a three-enzyme sequential cascade was realized by site-specifically immobilizing DNA-conjugated amylase, maltase, and glucokinase on a self-assembled DNA origami triangle. The kinetics of seven different enzyme configurations were evaluated experimentally and compared to simulations of optimized activity. A 30-fold increase in the pathway's kinetic activity was observed for enzymes assembled to the DNA. Detailed kinetic analysis suggests that this catalytic enhancement originated from increased enzyme stability and a localized DNA surface affinity or hydration layer effect and not from a directed enzyme-to-enzyme channeling mechanism. Nevertheless, the approach used to construct this pathway still shows promise toward improving other more elaborate multienzymatic cascades and could potentially allow for the custom synthesis of complex (bio)molecules that cannot be realized with conventional organic chemistry approaches.
The Autolytic Enzyme LytA of <i>Streptococcus pneumoniae</i> Is Not Responsible for Releasing Pneumolysin (2001)

It was previously proposed that autolysin's primary role in the virulence of pneumococci was to release pneumolysin to an extracellular location. This interpretation came into question when pneumolysin was observed to be released in significant amounts from some pneumococci during log-phase growth, because autolysis was not believed to occur at this time. We have reexamined this phenomenon in detail for one such strain, WU2. This study found that the extracellular release of pneumolysin from WU2 was not dependent on autolysin action. A mutant lacking autolysin showed the same pattern of pneumolysin release as the wild-type strain. Addition of mitomycin C to a growing WU2 culture did not induce lysis, indicating the absence of resident bacteriophages that could potentially harbor lytA-like genes. Furthermore, release of pneumolysin was unaltered by growth in 2% choline, a condition which is reported to inactivate autolysin, as well as most known pneumococcal phage lysins. Profiles of total proteins in the cytoplasm and in the supernatant media supported the hypothesis that release of pneumolysin is independent of pneumococcal lysis. Finally, under some infection conditions, mutations in pneumolysin and autolysin had different effects on virulence.
Fluid Flow at Branching Junctions (2015)

&lt;p&gt;The flow of fluids at branching junctions plays important kinematic and dynamic roles in most biological and industrial flow systems. The present paper highlights some key issues related to the flow of fluids at these junctions with special emphasis on the biological flow networks particularly blood transportation vasculature.&lt;/p&gt;
Comparison of the activities of protein disulphide-isomerase and thioredoxin in catalysing disulphide isomerization in a protein substrate (1991)

1. The activities of protein disulphide-isomerase (PDI) and thioredoxin in catalysing disulphide bond isomerization in a protein substrate were compared by using the standard assay, namely the re-activation of 'scrambled' RNAase. 2. The specific activity of PDI was 25-fold greater than that of thioredoxin. 3. The greater efficiency of PDI compared with thioredoxin is considered to be due more to the presence of multiple catalytic domains in PDI than to differences in their active-site sequences. 4. Data and procedures were defined for expressing enzyme activity in standard units, i.e. mumol of active RNAase generated/min.
Immunogenicity and Efficacy of Flagellin-Envelope Fusion Dengue Vaccines in Mice and Monkeys (2015)

The envelope (E) protein of flaviviruses includes three domains, EI, EII, and EIII, and is the major protective antigen. Because EIII is rich in type-specific and subcomplex-specific neutralizing epitopes and is easy to express, it is particularly attractive as a recombinant vaccine antigen. VaxInnate has developed a vaccine platform that genetically links vaccine antigens to bacterial flagellin, a Toll-like receptor 5 ligand. Here we report that tetravalent dengue vaccines (TDVs) consisting of four constructs, each containing two copies of EIII fused to flagellin (R3.2x format), elicited robust and long-lived neutralizing antibodies (geometric mean titers of 200 to 3,000), as measured with a 50% focus reduction neutralization test (FRNT50). In an immunogenicity study, rhesus macaques (n = 2) immunized subcutaneously with 10 μg or 90 μg of TDV three or four times, at 4- to 6-week intervals, developed neutralizing antibodies to four dengue virus (DENV) serotypes (mean post-dose 3 FRNT50 titers of 102 to 601). In an efficacy study, rhesus macaques (n = 4) were immunized intramuscularly with 16 μg or 48 μg of TDV or a placebo control three times, at 1-month intervals. The animals that received 48-μg doses of TDV developed neutralizing antibodies against the four serotypes (geometric mean titers of 49 to 258) and exhibited reduced viremia after DENV-2 challenge, with a group mean viremia duration of 1.25 days and 2 of 4 animals being completely protected, compared to the placebo-treated animals, which all developed viremia, with a mean duration of 4 days. In conclusion, flagellin-EIII fusion vaccines are immunogenic and partially protective in a nonhuman primate model.
3-D Printing of Elements in Frequency Selective Arrays (2014)

3-D printing is a technology that enables the fabrication of complex objects directly from a digital model. Folding the elements of Frequency Selective arrays in three dimensions gives a significant reduction in the resonant frequency for a given cell dimension, and such structures are candidates for additive manufacture. The aim in this paper is to demonstrate by example the development of novel electromagnetic structures that could be fabricated in parallel and integral with the additive manufacture of buildings, for electromagnetic architecture control. The principle is illustrated with two new geometries based on dipole and loop elements. The cores of these structures were fabricated with a 3-D printer that uses a plaster-based material. Theoretical and experimental results confirm the operation of the surfaces within the UHF frequency band.
Status of monopropellant hydrazine technology (1968)

Hydrazine properties, catalysts for hydrazine decomposition, catalytic reaction chambers, and monopropellant hydrazine thrustor
Fabrication of Thin Dielectric Films with Low Internal Stresses (1970)

Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Peer Review Share Icon Share Twitter Facebook Reddit LinkedIn Tools Icon Tools Reprints and Permissions Cite Icon Cite Search Site Citation Richard J. Scheuerman; Fabrication of Thin Dielectric Films with Low Internal Stresses. J. Vac. Sci. Technol. 1 January 1970; 7 (1): 143–146. https://doi.org/10.1116/1.1315777 Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search Dropdown Menu toolbar search search input Search input auto suggest filter your search All ContentAVS: Science & Technology of Materials Interfaces and ProcessingJournal of Vacuum Science and Technology Search Advanced Search |Citation Search
Hydrazinderivate und ihre Wirksamkeit gegenüber Mycobacterium tuberculosis (1952)

Hydrazide aliphatischer und isocyclischer Carbonsäuren sowie ihre Kondensationsverbindungen mit Oxoverbindungen zeigen in vitro tuberkulostatische Wirksamkeit. Auf Grund systematischer Untersuchungen wird gezeigt, daß Hydrazinderivate der allgemeinen Formel das Wachstum von Mycobacterium tuberculosis besonders gut hemmen. Für die Hemmwirkung ist der Molekülteil von besonderer Bedeutung, während modifizierenden Einfluß ausübt.
Schwefel‐Stickstoff‐Fluorverbindungen. X. Darstellung und Eigenschaften von SNF und NSF<sub>3</sub> (1961)

Abstract Bei der Reaktion von S 4 N 4 mit AgF 2 in CCl 4 entstehen neben zahlreichen anderen flüchtigen Verbindungen SNF und NSF 3 . SNF ist auch bei der thermischen Zersetzung von S 4 N 4 F 4 in CCl 4 , NSF 3 durch Fluorierung von SNF mit AgF 2 zu gewinnen. SNF : Fp.: −89°C; Kp.: +0,4 ± 2°C. Molare Verdampfungsenthalpie beim Siedepunkt 6052 ± 30 cal; Troutonsche Konstante: 22,1. NSF 3 : Fp.: −72,6° ± 0,5°C; Kp.: −27,1 ± 0,1°C. Molare Verdampfungsenthalpie beim Siedepunkt 5526 ± 50 cal; Troutonsche Konstante 22,5. SNF ist unbeständig. Die Hydrolyse mit H 2 O verläuft über OSNH quantitativ zu SO , F− und NH . Mit BF 3 treten farblose Kristalle, vermutlich SNF · BF 3 , auf. Chlorgas gibt neben anderen Produkten gasförmiges SNCl. NaJ wird zu J 2 oxydiert. NSF 3 ist sehr beständig; es hydrolysiert nicht mit verd. Säuren. Natronlauge gibt H 2 NSO ‐ und F − ‐Ionen. Mit BF 3 entstehen farblose Kristalle NSF 3 · BF 3 . Metallisches Natrium reagiert mit NSF 3 erst bei starkem Erhitzen. Bei der thermischen Zersetzung in Glasgefäßen bei 500°C beobachtet man S, SO 2 , N 2 , SiF 4 und Metallfluoride.
Improved QRM-ML detection with candidate selection for MIMO multiplexing systems (2007)

This paper proposes an improved QR decomposition associated M algorithm for maximum-likelihood detection (QRM-ML) with candidate selection in multiple input multiple output (MIMO) multiplexing systems. In the proposed algorithm, only the points falling into a sub-set of constellation are selected as the candidates for each transmitted signal and included in the squared Euclidean distance calculation. Unlike the existing algorithms where the sub-set is fixed based on quadrant, the sub-set here is determined by the circle with center at the signal estimate and a pre-determined radius. By computer simulations, it is shown that the proposed QRM-ML algorithm can achieve the performance close to that of the existing QRM-ML algorithms with significantly reduced complexity.
Removing T-cell epitopes with computational protein design (2014)

Immune responses can make protein therapeutics ineffective or even dangerous. We describe a general computational protein design method for reducing immunogenicity by eliminating known and predicted T-cell epitopes and maximizing the content of human peptide sequences without disrupting protein structure and function. We show that the method recapitulates previous experimental results on immunogenicity reduction, and we use it to disrupt T-cell epitopes in GFP and Pseudomonas exotoxin A without disrupting function.
LAL Regulators SCO0877 and SCO7173 as Pleiotropic Modulators of Phosphate Starvation Response and Actinorhodin Biosynthesis in Streptomyces coelicolor (2012)

LAL regulators (Large ATP-binding regulators of the LuxR family) constitute a poorly studied family of transcriptional regulators. Several regulators of this class have been identified in antibiotic and other secondary metabolite gene clusters from actinomycetes, thus they have been considered pathway-specific regulators. In this study we have obtained two disruption mutants of LAL genes from S. coelicolor (Δ0877 and Δ7173). Both mutants were deficient in the production of the polyketide antibiotic actinorhodin, and antibiotic production was restored upon gene complementation of the mutants. The use of whole-genome DNA microarrays and quantitative PCRs enabled the analysis of the transcriptome of both mutants in comparison with the wild type. Our results indicate that the LAL regulators under study act globally affecting various cellular processes, and amongst them the phosphate starvation response and the biosynthesis of the blue-pigmented antibiotic actinorhodin. Both regulators act as negative modulators of the expression of the two-component phoRP system and as positive regulators of actinorhodin biosynthesis. To our knowledge this is the first characterization of LAL regulators with wide implications in Streptomyces metabolism.
New Chitosan-Degrading Strains That Produce Chitosanases Similar to ChoA of <i>Mitsuaria chitosanitabida</i> (2005)

The betaproteobacterium Mitsuaria chitosanitabida (formerly Matsuebacter chitosanotabidus) 3001 produces a chitosanase (ChoA) that is classified in glycosyl hydrolase family 80. While many chitosanase genes have been isolated from various bacteria to date, they show limited homology to the M. chitosanitabida 3001 chitosanase gene (choA). To investigate the phylogenetic distribution of chitosanases analogous to ChoA in nature, we identified 67 chitosan-degrading strains by screening and investigated their physiological and biological characteristics. We then searched for similarities to ChoA by Western blotting and Southern hybridization and selected 11 strains whose chitosanases showed the most similarity to ChoA. PCR amplification and sequencing of the chitosanase genes from these strains revealed high deduced amino acid sequence similarities to ChoA ranging from 77% to 99%. Analysis of the 16S rRNA gene sequences of the 11 selected strains indicated that they are widely distributed in the beta and gamma subclasses of Proteobacteria and the Flavobacterium group. These observations suggest that the ChoA-like chitosanases that belong to family 80 occur widely in a broad variety of bacteria.
A fast non-contact imaging photoplethysmography method using a tissue-like model (2018)

Imaging photoplethysmography (iPPG) allows non-contact, concomitant measurement and visualization of peripheral blood flow using just an RGB camera. Most iPPG methods require a window of temporal data and complex computation, this makes real-time measurement and spatial visualization impossible. We present a fast,“window-less”, non-contact imaging photoplethysmography method, based on a tissue-like model of the skin, that allows accurate measurement of heart rate and heart rate variability parameters. The error in heart rate estimates is equivalent to state-of-the-art techniques and computation is much faster.
Corrupción, delito y crisis en la Administración de Justicia (2013)

En este trabajo se contempla el grave deterioro al que ha llevado la corrupcion. Estan involucrados varios partidos politicos, algunas instituciones y otros sectores. Los ciudadanos desconfian de la Justicia, la consideran politizada, y que los politicos y otros poderosos que han cometido delitos reciben mejor trato que al resto de la poblacion. Hay organos superiores de la Administracion de Justicia que deben desaparecer.
CONDENSATION OF ALICYCLIC KETONES WITH UREA AND THIOUREA (1964)

The previous assignment of a cis conformation to cyclohexyl 2-carbamylcyclohexylamine, which was prepared by the condensation of urea with cyclohexanone, has been confirmed by equilibration in the presence of potassium t-butoxide. The failure of 4-t-butylcyclohexyl 2-carbamyl-4-t-butylcyclohexylamine to equilibrate under the same conditions is discussed in relation to its structure. 1,2,3,4,5,6,7,8-Octahydroacridine was prepared by the condensation of 2,2′-methylene-bis-cyclohexanone with urea.
Reducing the environmental sensitivity of cepstral features for speaker recognition (2002)

This paper investigates the robustness of cepstral based features with respect to additive noise, and details two methods of increasing the robustness with minimal need for a-priori knowledge of the noise statistics. The first approach is a form of noise masking which adds a fixed offset to the linear spectral estimate. The second is a form of sub-band filtering, again in the linear domain, which estimates the dynamic content of the speech using Fourier transforms. This avoids negative values normally inherent in such filtering and which presents difficulties in deriving log estimates. Both methods are shown to provide useful levels of robustness to additive noise, for example, speaker identification error rates in SNR mis-matched conditions of 15 dB are reduced from 60.5% for standard mel cepstra to 13.8% and 24.1% for the two approaches respectively, a relative reduction in error of 77% and 60.1%.
Chemistry of cephalosporin antibiotics. XV. Transformations of penicillin sulfoxide. Synthesis of cephalosporin compounds (1969)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTChemistry of cephalosporin antibiotics. XV. Transformations of penicillin sulfoxide. Synthesis of cephalosporin compoundsRobert B. Morin, Bill G. Jackson, Richard A. Mueller, Edward R. Lavagnino, W. B. Scanlon, and Sandra L. AndrewsCite this: J. Am. Chem. Soc. 1969, 91, 6, 1401–1407Publication Date (Print):March 1, 1969Publication History Published online1 May 2002Published inissue 1 March 1969https://pubs.acs.org/doi/10.1021/ja01034a023https://doi.org/10.1021/ja01034a023research-articleACS PublicationsRequest reuse permissionsArticle Views1045Altmetric-Citations146LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts