gebhart/patrepeval huggingface dataset:
Stichwortverzeichnis (2019)

You have accessSQLNov 2019StichwortverzeichnisRalf AdamsRalf Adamshttps://doi.org/10.3139/9783446462748.bmSectionsAboutPDF ToolsAdd to FavoritesDownload CitationTrack CitationsCopy LTI LinkPDF ShareFacebookTwitterEmailLinkedIn previous chapter FiguresReferencesRelatedDetails 2019Pages: 637-646Print ISBN: 978-3-446-46110-9eISBN: 978-3-446-46274-8 Copyright & Permissions© 2020 Carl Hanser Verlag GmbH & Co. KGPDF DownloadLoading ...
Preclinical Evaluation of the Antifolate QN254, 5-Chloro-<i>N</i>′6′-(2,5-Dimethoxy-Benzyl)-Quinazoline-2,4,6-Triamine, as an Antimalarial Drug Candidate (2010)

Drug resistance against dihydrofolate reductase (DHFR) inhibitors-such as pyrimethamine (PM)-has now spread to almost all regions where malaria is endemic, rendering antifolate-based malaria treatments highly ineffective. We have previously shown that the di-amino quinazoline QN254 [5-chloro-N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine] is active against the highly PM-resistant Plasmodium falciparum V1S strain, suggesting that QN254 could be used to treat malaria in regions with a high prevalence of antifolate resistance. Here, we further demonstrate that QN254 is highly active against Plasmodium falciparum clinical isolates, displaying various levels of antifolate drug resistance, and we provide biochemical and structural evidence that QN254 binds and inhibits the function of both the wild-type and the quadruple-mutant (V1S) forms of the DHFR enzyme. In addition, we have assessed QN254 oral bioavailability, efficacy, and safety in vivo. The compound displays favorable pharmacokinetic properties after oral administration in rodents. The drug was remarkably efficacious against Plasmodium berghei and could fully cure infected mice with three daily oral doses of 30 mg/kg. In the course of these efficacy studies, we have uncovered some dose limiting toxicity at higher doses that was confirmed in rats. Thus, despite its relative in vitro selectivity toward the Plasmodium DHFR enzyme, QN254 does not show the adequate therapeutic index to justify its further development as a single agent.
New syntheses of functional arenesulfonyl azides (1975)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNew syntheses of functional arenesulfonyl azidesHenri Ulrich, F. A. Stuber, B. Tucker, and A. A. R. SayighCite this: J. Org. Chem. 1975, 40, 6, 802–804Publication Date (Print):March 1, 1975Publication History Published online1 May 2002Published inissue 1 March 1975https://pubs.acs.org/doi/10.1021/jo00894a032https://doi.org/10.1021/jo00894a032research-articleACS PublicationsRequest reuse permissionsArticle Views180Altmetric-Citations4LEARN 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
A low cost direct current source for the laboratory (1961)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA low cost direct current source for the laboratoryW. Robert. Barnard and Ray Woodriff Cite this: J. Chem. Educ. 1961, 38, 10, 521Publication Date (Print):October 1, 1961Publication History Received3 August 2009Published online1 October 1961Published inissue 1 October 1961https://doi.org/10.1021/ed038p521RIGHTS & PERMISSIONSArticle Views65Altmetric-Citations1LEARN 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 InReddit PDF (500 KB) Get e-Alerts Get e-Alerts
A<i>Hin</i>dIII RFLP for the HPRT pseudogene on chromosome 3 (HPRTP1) (1987)

Journal Article A HindIII RFLP for the HPRT pseudogene on chromosome 3 (HPRTP1) Get access A. Dobrovic, A. Dobrovic Search for other works by this author on: Oxford Academic PubMed Google Scholar P. Gareau, P. Gareau Search for other works by this author on: Oxford Academic PubMed Google Scholar A.-M. Seifert, A.-M. Seifert 1Département des Sciences Biologiques, Université du Québec à MontréalMontréal, Canada Search for other works by this author on: Oxford Academic PubMed Google Scholar K. Messing, K. Messing 1Département des Sciences Biologiques, Université du Québec à MontréalMontréal, Canada Search for other works by this author on: Oxford Academic PubMed Google Scholar W.E.C. Bradley W.E.C. Bradley Search for other works by this author on: Oxford Academic PubMed Google Scholar Nucleic Acids Research, Volume 15, Issue 3, 11 February 1987, Page 1346, https://doi.org/10.1093/nar/15.3.1346 Published: 11 February 1987
Influence of Methylproline Isomers upon Neoviridogrisein Synthesis (1982)

Influence of positional and stereoisomers of methylproline on the biosynthesis of neoviridogrisein (NVG) by Streptomyces griseoviridus P8648 was investigated. 3-(dl-cis + trans)- and 5-(d-cis + l-trans)-Methylprolines inhibited NVG synthesis, but they did not affect the cell growth. When these imino acids were added to cultures of S. griseoviridus P8648, there occurred no production of NVG homologues. In the presence of 4-methylproline (d-cis + l-trans), the organism synthesized a new NVG, designated NVG-MP, in which the imino acid moiety was replaced by 4-methylproline (d-cis). The antimicrobial activity of NVG-MP was compared with those of NVG II and viridogrisein (VG).
Intraventricular rhabdoid tumor: first case report in a young adult (1997)

info:eu-repo/semantics/nonPublished
Use of Electrodeless Discharge Lamps in the Analysis of Atomic Spectra (1963)

The application of electrodeless discharge lamps in obtaining the information necessary for the analysis of the first and second spectra of lanthanide and actinide elements is discussed. It is shown how differentiation of neutral atom and first ion lines, self-reversal, and Zeeman-effect observations may be procured using these lamps as the sole source. The procedures are illustrated by studies on Cm, Gd, and Dy.
Anosognosia and confabulation during the Wada test (1997)

Feinberg et al. proposed that right-hemisphere-damaged stroke patients with anosognosia for hemiplegia (AHP) confabulate seeing stimuli on the left side but those without AHP admit to having inadequate visual information. This study examines the relationship between AHP and confabulation using selective anesthesia of the cerebral hemispheres. Seventeen patients with intractable epilepsy were tested during intracarotid methohexital infusion. For half of the trials, subjects were stimulated on their paretic hand with a material (sandpaper, metal, or cloth), and for the remaining trials they were not stimulated. The subjects were trained to use a pointing response to indicate if they been stimulated and the type of material they had felt. Admission of uncertainty was defined as pointing to a question mark. Confabulation was defined as any material response to a no-touch trial. During anesthesia of either hemisphere, subjects with and without AHP confabulated responses. The AHP and non-AHP groups did not differ in admission of uncertainty. Our results support the postulate that confabulation and AHP are independent disorders, and therefore confabulation cannot fully account for AHP.
Sequential Deconjugative Electrophilic Fluorination/Cross-Metathesis: Toward the Synthesis of Fluoro Analogues of Biologically Active Compounds (2015)

For the first time, a deconjugative electrophilic fluorodesilylation reaction was accomplished. γ-Silyl butenamides were treated with Selectfluor to provide α-fluoro-β,γ-unsaturated amides. Other sources of electrophilic fluorine were not efficient or gave protodesilylated side products. The electrophilic fluorodesilylation reaction was followed by a ruthenium-catalyzed cross-metathesis of the resulting functionalized allylic fluoride. The fluorodesilylation/cross-metathesis sequence is ideal for the synthesis of fluoro analogues of symbior­amide.
An Age Adjusted Comorbidity Index to Predict Long-Term, Other Cause Mortality in Men with Prostate Cancer (2015)

The age adjusted PCCI strongly stratifies the risk of long-term, other cause mortality. It may be incorporated into shared decision making to decrease overtreatment of older and chronically ill men with prostate cancer.
Epistemologies of Resistance: Pluralism and Communities of Epistemic Criticism (2015)

Needing Not to Know: Ignorance, Innocence, Denials and Discourse" focuses on a difficulty in the pedagogy of social justice that Barbara Applebaum frames in the following way: "If exposure to others is already distorted by meta-insensitivities that are socially supported, how can exposure to alternative views be a remedy for meta-ignorance?"The difficulty is clear and resonates with a long-standing problem in education that can be traced back to the Meno and other aporetic dialogues.The general pedagogical difficulty of which this is a specific form runs something like this: (1) Learning requires openness to new experiences; (2) ignorance is the state of not being open to new experiences; (3) therefore, the ignorant person cannot learn.One could view Socrates' torpedo-fish rhetoric as an attempt to shake off this paradox and pierce the veil of ignorance or as a sign of a deep and even metaphysically intractable problem for education.In Plato's Republic, this paradox plays a central role, as it gives license to invoke philosophical insight as a transcendental solution to this paradox.If wisdom cannot be taught, but only directly perceived through transcendental insight, then there is no possibility for a democratic social arrangement.The best political arrangement grants authority to the philosopher, follows her lead, and hopes for the best.
A Longitudinal Study of Thought Disorder in Manic Patients (1986)

To study the persistence of thought disorder in manic patients, 34 manic patients were compared with 30 schizophrenic and 30 nonpsychotic patients on four indexes of thought pathology at two phases of disorder: during the acute inpatient phase and one year after hospitalization. Patients were also compared with a control sample of 34 normal subjects. The data indicated that during the acute in hospital phase, both manic and schizophrenic patients were severely thought disordered; at follow-up, a subsample of manic patients showed severe thought disorder; despite the severe thought disorder found at follow-up in some manic and schizophrenic patients, both groups showed a significant reduction of thought pathology at follow-up; and there was a trend for a larger reduction of thought disorder in manic than in schizophrenic patients. The difference, however, was not significant when initial levels of severity were controlled.
Synthesis of New Compounds Containing the 2,3‐Dihydro[1,4]dioxino[2,3‐b]pyridine Heterocyclic System as a Substructure. (2003)

Abstract For Abstract see ChemInform Abstract in Full Text.
THE 1‐CYANONAPHTHALENE EXCIMER IN HOMOGENEOUS AND MICELLAR SOLUTIONS (1980)

Abstract— An excimer of 1‐cyanonaphthalene is produced in homogeneous organic solvents and in micelle containing detergent solutions. From solvent effects in homogeneous solution it is concluded that the excimer is relatively polar (dipole moment ∼ 4D). From a comparison with emission from that observed in homogeneous solvents, it is concluded that 1‐cyanonaphthalene is solubilized mainly in the Stern Layer of sodium dodecyl sulfate (SDS) and hexadecyltrimethyl ammonium bromide (HDTBr) micelles. The influence of variation of detergent concentration on the excimer to monomer emission ratio and the influence of NaCl concentration on the excimer to monomer emission ratio have been determined. Excimer formation is shown to be a convenient method for determination of the Kraft point of SDS solutions.
Optimal steering of a linear stochastic system to a final probability distribution, part II (2014)

We consider the problem of minimum energy steering of a linear stochastic system to a final prescribed distribution over a finite horizon and to maintain a stationary distribution over an infinite horizon. We present sufficient conditions for optimality in terms of a system of dynamically coupled Riccati equations in the finite horizon case and algebraic in the stationary case. We then address the question of feasibility for both problems. For the finite-horizon case, provided the system is controllable, we prove that without any restriction on the directionality of the stochastic disturbance it is always possible to steer the state to any arbitrary Gaussian distribution over any specified finite time-interval. For the stationary infinite horizon case, it is not always possible to maintain the state at an arbitrary Gaussian distribution through constant state-feedback. It is shown that covariances of admissible stationary Gaussian distributions are characterized by a certain Lyapunov-like equation. We finally present an alternative to solving the system of coupled Riccati equations, by expressing the optimal controls in the form of solutions to (convex) semi-definite programs for both cases. We conclude with an example to steer the state covariance of the distribution of inertial particles to an admissible stationary Gaussian distribution over a finite interval, to be maintained at that stationary distribution thereafter by constant-gain state-feedback control.
Reactions of Zirconacyclopentadienes with CO, CN, and NN Moieties with Electron-Withdrawing Groups:  Formation of Six-Membered Heterocycles (2002)

Reactions of zirconacyclopentadienes with diethyl ketomalonate gave alpha-pyrans in excellent yields in the presence of BiCl3. In the absence of BiCl3, zirconacyclopentadienes did not react with diethyl ketomalonate. Tetraphenylzirconacyclopentadiene reacted with diethyl ketomalonate in the presence of BiCl3 to give a ring-opening product, dienolic ether, in 53% yield. The structures of the alpha-pyran prepared from diethyldiphenylzirconacyclopentadiene and the ring-opening product were determined by X-ray analysis. When oximinosulfonate was added to tetraethylzirconacyclopentadiene in THF at -78 degrees C, 3,4,5,6-tetraethylpyridine-2-carbonitrile was obtained in 95% yield within 10 min. The structure of the product was confirmed by X-ray analysis. When tetraethylzirconacyclopentadiene was treated with azodicarboxylate in the presence of 2 equiv of CuCl at -78 degrees C, 1,2-dialkoxycarbonyl-3,4,5,6-tetraethyl-1,2-dihydropyridazine derivatives were obtained. The structure of one of dihydropyridazine was also confirmed by X-ray analysis.
Experimental testing of the Preisach modeling of superconducting hysteresis (2000)

Extensive experimental testing of the Preisach modeling of superconducting hysteresis is reported. This testing demonstrates the remarkable accuracy of the Preisach model in predicting various branches of superconducting hysteresis for various past histories and in the wide range of temperatures.
Monitoring Toxic Ionic Liquids in Zebrafish (<i>Danio rerio</i>) with Desorption Electrospray Ionization Mass Spectrometry Imaging (DESI-MSI) (2016)

Ambient mass spectrometry imaging has become an increasingly powerful technique for the direct analysis of biological tissues in the open environment with minimal sample preparation and fast analysis times. In this study, we introduce desorption electrospray ionization mass spectrometry imaging (DESI-MSI) as a novel, rapid, and sensitive approach to localize the accumulation of a mildly toxic ionic liquid (IL), AMMOENG 130 in zebrafish (Danio rerio). The work demonstrates that DESI-MSI has the potential to rapidly monitor the accumulation of IL pollutants in aquatic organisms. AMMOENG 130 is a quaternary ammonium-based IL reported to be broadly used as a surfactant in commercialized detergents. It is known to exhibit acute toxicity to zebrafish causing extensive damage to gill secondary lamellae and increasing membrane permeability. Zebrafish were exposed to the IL in a static 96-h exposure study in concentrations near the LC<sub>50</sub> of 1.25, 2.5, and 5.0 mg/L. DESI-MS analysis of zebrafish gills demonstrated the appearance of a dealkylated AMMOENG 130 metabolite in the lowest concentration of exposure identified by a high resolution hybrid LTQ-Orbitrap mass spectrometer as the trimethylstearylammonium ion, [C<sub>21</sub>H<sub>46</sub>N]<sup>+</sup>. With DESI-MSI, the accumulation of AMMOENG 130 and its dealkylated metabolite in zebrafish tissue was found in the nervous and respiratory systems. AMMOENG 130 and the metabolite were capable of penetrating the blood brain barrier of the fish with significant accumulation in the brain. Hence, we report for the first time the simultaneous characterization, distribution, and metabolism of a toxic IL in whole body zebrafish analyzed by DESI-MSI. This ambient mass spectrometry imaging technique shows great promise for the direct analysis of biological tissues to qualitatively monitor foreign, toxic, and persistent compounds in aquatic organisms from the environment. Graphical Abstract ᅟ.
Propofol and its solvent effect on the non-specific branch of the immune system (2000)

European Society of Anaesthesiologists; 8th Annual Meeting with the Austrian International Congress; Vienna, Austria, 1-4 April 2000
High-frequency properties of SrTiO3 thin-film capacitors fabricated on polymer-coated alloy substrates (1998)

Low-temperature (200 °C) sputter deposition of SrTiO3 (STO) thin films by using ultrahigh-density ceramic target enabled us to fabricate capacitors on polyimide-isoindroquinazoline dione (PIQ)- or benzocyclobutene (BCB)-coated alloy substrates. Complex impedances of the capacitors were analyzed. Capacitances of the 0.01 mm2 area capacitors with 200-nm-thick STO films were around 22 pF and were not dependent on frequency up to 8 GHz. Leakage-current densities of the films were lower than 10−6 A/cm2 at an applied voltage of 10 V and dielectric loss tangents were lower than 10−6.
Elucidation of Shimura’s Reduction Parameter for the First Ligand Field Band Components of Cobalt(III) and Chromium(III) Mixed Ligand Complexes (1990)

Abstract Elucidation was made for Shimura’s recently proposed reduction parameter, which enables us to improve the prediction of the first absorption band components from Yamatera’s rule, in terms of the angular overlap model(AOM) parameterization for cobalt(III) and chromium(III) mixed ligand complexes. From the configuration interaction between the degenerate components and in view of the empirical relation for the eσa and eσb AOM parameters as revealed recently in the nondegenerate component of trans-[Cra4b2] type complexes, Shimura’s empirical reduction parameter α was elucidated semiquantitatively in relation with the difference between the eσ parameter values for the a and b ligands, Δ′σb=3(eσb−eσa); the larger the Δ′σb the smaller the reduction parameter α, and vice versa.
Microstructure and properties of Al{sub 2}O{sub 3}/Al composites formed by in situ reaction of aluminum and mullite (1995)

Novel property Al{sub 2}O{sub 3}/Al composites have been produced by reactive metal penetration, which includes in situ reaction of molten Al with dense mullite ceramic performs. Molten aluminum reduces mullite to produce alumina and elemental silicon following the reaction, 3 Al{sub 6}Si{sub 2}O{sub 13} + (8 + x) Al {r_arrow} 13 Al{sub 2}O{sub 3} + (x) Al + (6 {minus} y) Si {minus} (y) Si{sub (lost to melt)}. Si diffusion out of the system produces an Al{sub 2}O{sub 3}/Al composite containing up to 30% by volume Al. Al{sub 2}O{sub 3}/Al composites produced by in situ reaction of aluminum and mullite have improved physical properties relative to the dense mullite ceramic perform. A rigid alumina skeleton dominates composite physical properties such as Young`s modulus (E), hardness (Hv), and coefficient of thermal expansion (CTE), while the interpenetrating ductile Al metal phase contributes to improved composite fracture toughness (K{sub IC}). Composite K{sub IC} increases with increasing metal content, x, and microstructural analysis of fracture surfaces of metal-ceramic composites produced by reactive metal penetration show visible evidence of the ductile metal failure.
Specifications for Computer Networks for Support of Cooperative Ventures Between Universities and Public Schools (1991)

No abstract available for this article.
A generic in-place transformation-based approach to structured model co-evolution (2010)

In MDE not only models but also metamodels are subject to evolution.More specifically, they need to be adapted to correct errors, support new and/orupdate language features. The direct consequence of such evolutionary steps comprisesthe problem of managing the co-evolution of existing model instances, whichmay no longer conform to the new metamodel version. This model migration isintrinsically complex and results in a time-consuming and error-prone process if noadequate support is provided. For tackling this problem, we introduce a new techniqueto guide the user in solving migration issues in a step-wise manner. The aimsare manifold, notably the simplification of the migration specification, the reductionof the effort for the evolver, the control of user intervention, and the optimizationof the migration execution itself by allowing in-place adaptation of the existing instances.