gebhart/patrepeval huggingface dataset:
COX-2 inhibitors with a methylsulfoxide pharmacophore (2005)

AbstractNovel methylsulfoxide analogues, of known selective cyclooxygenase-2 (COX-2) inhibitors, with a methylsulfone moiety are claimed as COX-2 inhibitors. The inhibitors are useful for the treatment of COX-2-mediated disorders comprising inflammation and inflammation-associated disorders. The clinical applicability for development of the claimed sulfoxide analogues as COX-2 inhibitors is eval-uated against the car-diovascular and gastrointestinal safety.Keywords:: cardiovascular safetycyclooxygenase-2 (COX-2)gastrointestinal safetyprodrug
Use of a Potent, Long Acting Agonist of Gonadotropin-Releasing Hormone in the Treatment of Precocious Puberty* (1986)

Studies utilizing the administration of GnRH in various GnRH-deficient models have revealed the critical importance of the dose and mode of delivery of this releasing factor in determining the subsequent pituitary response. Chronic administration of long acting GnRH agonists (GnRHa), like continuous infusion of high doses of the native peptide, results in suppression of pituitary gonadotropin secretion. This selective and reversible suppression of gonadotropin secretion suggested several therapeutic applications for these analogs, particularly in the treatment of central precocious puberty (CPP), a disorder for which the previously available therapies lacked uniform efficacy and were associated with potential side effects. In our series, 74 children with CPP have been treated during the last 5 yr with the potent GnRH agonist, [D-Trp6, Pro9-ethylamide(NEt)]GnRH. Having selected a dose and route of administration that produced uniform suppression of spontaneous and stimulated pituitary gonadotropin secretion, GnRHa therapy resulted in a fall of gonadal sex steroid levels into the prepubertal range, a halting or regression of secondary sexual development, and a complete cessation of menses. Growth velocity slowed during therapy, with this slowing more pronounced during prolonged treatment periods and among those patients with more advanced chronological and skeletal ages. Skeletal maturation was retarded to a greater degree than linear growth, with resultant increases in the predictions for adult stature. Moreover, these benefits have been achieved in the absence of significant side effects. Complete reversal of the suppression of gonadarche has followed discontinuation of therapy; however, patterns of growth and skeletal maturation after discontinuation of GnRHa administration remain to be characterized. Thus, the impact of GnRHa therapy on final height must await further longitudinal study. The selective nature of GnRHa suppression of gonadarche also permits an investigation of the natural history of adrenarche and its discrete influences upon skeletal growth and maturation. In addition, GnRHa therapy of CPP provides a unique opportunity to study the effects of gonadal sex steroids on GH secretion and somatomedin-C (Sm-C) generation during sexual maturation. Finally, the detailed characterization of children with precocious puberty has helped to define more precisely a subset of patients whose precocity occurs in the absence of demonstrable gonadotropin secretion.(ABSTRACT TRUNCATED AT 400 WORDS)
Carbon dioxide adsorption based on porous materials (2021)

Global warming due to the high concentration of anthropogenic CO<sub>2</sub> in the atmosphere is considered one of the world's leading challenges in the 21<sup>st</sup> century as it leads to severe consequences such as climate change, extreme weather events, ocean warming, sea-level rise, declining Arctic sea ice, and the acidification of oceans. This encouraged advancing technologies that sequester carbon dioxide from the atmosphere or capture those emitted before entering the carbon cycle. Recently, CO<sub>2</sub> capture, utilizing porous materials was established as a very favorable route, which has drawn extreme interest from scientists and engineers due to their advantages over the absorption approach. In this review, we summarize developments in porous adsorbents for CO<sub>2</sub> capture with emphasis on recent studies. Highly efficient porous adsorption materials including metal-organic frameworks (MOFs), zeolites, mesoporous silica, clay, porous carbons, porous organic polymers (POP), and metal oxides (MO) are discussed. Besides, advanced strategies employed to increase the performance of CO<sub>2</sub> adsorption capacity to overcome their drawbacks have been discoursed.
Homochiral Crystallization of Microporous Framework Materials from Achiral Precursors by Chiral Catalysis (2008)

While it is not uncommon to form chiral crystals during crystallization, the formation of bulk porous homochiral materials from achiral building units is rare. Reported here is the homochiral crystallization of microporous materials through the chirality induction effect of natural alkaloids. The resulting material possesses permanent microporosity and has a uniform pore size of 9.3 A.
Development of a functional ruthenium(ii) complex for probing hypochlorous acid in living cells (2014)

A functional ruthenium(ii) complex, [Ru(bpy)2(AN-bpy)](PF6)2 (bpy: 2,2'-bipyridine, AN-bpy: 4-methyl-4'-(4-amino-3-nitro-phenoxy-methylene)-2,2'-bipyridine), has been designed and synthesized as a turn-on luminescent probe for the imaging of hypochlorous acid (HOCl) in living cells. Due to the intramolecular photoinduced electron transfer (PET), the ruthenium(ii) complex itself is almost non-luminescent. However, it can specifically and rapidly react with HOCl in aqueous media to afford a highly luminescent derivative, [Ru(bpy)2(HM-bpy)](PF6)2 (HM-bpy: 4-hydroxymethyl-4'-methyl-2,2'-bipyridine), accompanied by a 110-fold luminescence enhancement. Taking advantage of high specificity and sensitivity, and excellent photophysical properties of the ruthenium(ii) complex probe, [Ru(bpy)2(AN-bpy)](PF6)2 was successfully applied to the luminescence imaging of the exogenous HOCl in living HeLa cells and the endogenous HOCl in porcine neutrophils. The results corroborate that indeed [Ru(bpy)2(AN-bpy)](PF6)2 is a useful luminescent probe for the monitoring of HOCl in biological systems.
Memory impairment after soman intoxication in rat: correlation with central neuropathology. Improvement with anticholinergic and antiglutamatergic therapeutics. (1999)

The effects of soman, a potent irreversible inhibitor of acetylcholinesterase, on central neuropathology in rats were studied in relation with subsequent spatial memory impairments. In a first step, it was found that, without treatment, neuropathology and learning impairment were observed only in rats which experienced convulsions. Then, treatment consisting of atropine sulfate, and/or TCP and/or NBQX was administered to intoxicated animals at infraanticonvulsant doses to obtain a graded subsequent neuropathology and to appreciate an eventual relation between neuropathology and spatial memory impairment. Thus, a correlation between neuropathology in the hippocampal CA1 region and spatial learning performance was found, the degradation of performance of rat being directly related to the amplitude of their neural damage. A threshold was emphasized : below a certain degree of neural loss, no memory impairment was found. Only treatment with tritherapy (atropine + TCP + NBQX) was able to improve the different parameters of spatial learning, despite no effect on the convulsions of the animals.
Amoeba-inspired algorithm for cognitive medium access (2014)

The “tug-of-war (TOW) model” is a unique parallel search algorithm for solving the multi-armed bandit problem (BP), which was inspired by the photoavoidance behavior of a single-celled amoeboid organism, the true slime mold Physarum polycephalum [1-4]. “The cognitive medium access (CMA) problem,” which refers to multiuser channel allocations of the cognitive radio, can be interpreted as a “competitive multi-armed bandit problem (CBP) [5, 6].” Unlike the normal BP, the CBP considers a competitive situation in which more than one user selects a channel whose reward probability (probability of which channel is free) varies depending on the number and combination of the selecting users as indicated in a payoff matrix. Depending on the payoff matrix, the CBP provides a hard problem instance in which the users should not be attracted to the Nash equilibrium to achieve the “social maximum,” which is the most desirable state to obtain the maximum total score (throughput) for all the users. In this study, we propose two variants of the TOW model (solid type and liquid type) for the CBP toward developing a CMA protocol using a distributed control in uncertain environments. Using the minimum CBP cases where both the users choose a channel from the two considered channels, we show that the performance of our solid-type TOW model is better than that of the well-known upper confidence bound 1 (UCB1)-tuned algorithm, particularly for the hard problem instances. The aim of this study is to explore how the users can achieve the social maximum in a decentralized manner. We also show that our liquid-type TOW model, which introduces direct interactions among the users for avoiding mutual collisions, makes it possible to achieve the social maximum for general CBP instances.
Characterization of enzyme immobilization in liposomes prepared from proliposomes (1996)

This study investigated the influence of ionic strength, liposome net charge and enzyme concentration on the immobilization of chymotrypsin in liposomes obtained from proliposomes. Depending on ionic strength and chymotrypsin concentration, immobilization efficiencies (IE) as high as 96 and 68% were obtained for liposomes prepared with Pro-lipo 3045 S and Pro-lipo 3080 S respectively. Increasing ionic strength and enzyme concentration resulted in a decrease in IE for both types of liposomes, and this was more pronounced for ionic strength. Relatively high amounts of chymotrypsin were found to be immobilized on the surface of the liposomes. Hydrophobic interactions between chymotrypsin and the hydrophobic tails of the phospholipids during liposome formation were probably responsible for this phenomenon.
El lenguaje en los SMS: la alfabetización de los jóvenes en el siglo XXI, ¿avance o retroceso? (2006)

El lenguaje de móviles está generando una revolución en el\n\t\t\t\t idioma, que sin prejuicios, pensamos, sería un cambio en el\n\t\t\t\t proceso de alfabetización de los jóvenes del siglo XXI, y por tanto\n\t\t\t\t un posible cambio que pudiera afectar a nuestra Lengua Española.\n\t\t\t\t Simplemente, mostramos algunas justificaciones de estos procesos\n\t\t\t\t y las leyes que rigen el lenguaje SMS, con ejemplos ilustrativos.
Power harvesting and telemetry in CMOS for implanted devices (2005)

Implanted sensors offer many advantages to study and monitor the human body. Wires or batteries often compromise their usefulness. We describe a telemetry chip that by inductive coupling supplies power to and transmits digital data from an implantable sensor. The same two coils are used to transmit both power and data. The chip fabricated in 0.5-/spl mu/m CMOS technology supplies 1.7 mA at 3.3 V, over a distance up to 25 mm between coils. Experiments emulating the effect of human tissue by introducing water bearing colloids between the two coils revealed a negligible loss of transfer efficiency. With modified Miller encoding, the data link attained 3 10/sup -5/ bit error rate at 10 kbps transmission speed over 25 mm distance. Repeated tests using the same colloids between coils resulted in a slight decrease in the signal to noise ratio of the data stream with increasing thickness.
Niobium–η-cyclopentadienyl compounds with imido and amido ligands derived from 2,6-dimethylaniline (2000)

The new niobium imido complex [Nb(η-C5H5){N(C6H3Me2-2,6)}Cl2] 1* has been prepared. Its reactions with anionic reagents lead to a series of alkyl and amido derivatives [Nb(η-C5H5){N(C6H3Me2-2,6)}MeCl] 2, [Nb(η-C5H5){N(C6H3Me2-2,6)}{NH(C6H3Me2-2,6)}Cl] 3, [Nb(η-C5H5){N(C6H3Me2-2,6)}{NH(C6H3Me2-2,6)}2] 4*, [Nb(η-C5H5)2{N(C6H3Me2-2,6)}Cl] 5, [Nb(η-C5H5)2{N(C6H3Me2-2,6)}Me] 6 and [Nb(η-C5H5){N(C6H3Me2-2,6)}{NH(C6H3Me2-2,6)}Me] 7*. Variable temperature NMR studies on the amido complexes 3, 4 and 7 are reported (* indicates the crystal structure has been determined).
Histone deacetylases are dysregulated in rheumatoid arthritis and a novel histone deacetylase 3–selective inhibitor reduces interleukin‐6 production by peripheral blood mononuclear cells from rheumatoid arthritis patients (2011)

HDAC activity is dysregulated in RA PBMCs and is a potential target for therapeutic intervention, as it is not affected by conventional anti-TNF treatment with etanercept. Both the selective and the nonselective HDAC inhibitors (MI192 and TSA, respectively) were found to regulate cytokine production from PBMCs, but their effects were cell type and compound specific. HDAC inhibitors have potential in the treatment of RA, and HDAC-selective inhibition may improve the therapeutic margin of safety; however, further clinical characterization and evaluation for adverse effects is needed.
On the implementation of a multi-equalizer (2005)

Nowadays, the use of equalizers in wireless telecommunication systems is facilitated by the evolution of microelectronic. It is now possible to implement more than one equalizer in a programmable circuit. In (Dumais et al., 2004), a multi-equalizer (MEQ) architecture has been presented. The results have shown an improvement in BER performances when the propagation environment is fluctuating. This paper presents the FPGA implementation results of a DFE/LTE multi-equalizer. Multi-equalizing or parallel selection of multiple equalizers outputs is achieved by the definition of a cooperation strategy between filters, an algorithmic validation of the architecture by numerical simulations and a FPGA implementation of the structure.
Sequence of a Complementary DNA from <i>Cucumis sativus</i> L. Encoding the Stearoyl-Acyl-Carrier Protein Desaturase (1991)

The stearoyl-ACP2 desaturase (EC 1.14.99.6) is responsible for introducing a cis double bond between carbons 9 and 10 ofstearoyl-ACP to form oleoyl-ACP (1) (Table I).Purification of the avocado enzyme and isolation of cDNA clones from Ricinus communis (castor) and Cucumis sativus L. (cucumber) and their corresponding amino acid sequences have recently been reported (2).Here we present the nucleotide sequence of a full-length cucumber cDNA (from plasmid pCSDl) and the deduced amino acid sequence of the open reading frame.The 396 amino acid open reading frames of the cucumber and the castor clones are 80.1% identical at the nucleotide level and 88. 1% identical at the amino acid level.ACKNOWLEDGMENT We thank Dr. J. Greenler and Dr. W. Becker for the generous gift of a
Chemical Characterization of Bromine Oxidized Potato Starch (1990)

Abstract Potato starch was oxidized with a neutral aqueous bromine solution at seven different levels of molar ratios of bromine/starch (1/40–5/1). The molecular weight distribution of the products obtained was analysed by gel permeation chromatography on two different agarose gels, Sepharose CL‐2B and Superose 6. A gradually increased fragmentation of the molecules with increased oxidation level was noticed. Some of the modified samples were debranched and the products obtained were analysed by gel permeation chromatography. For comparison amylose and waxy maize starch were also treated at the 1/20 and 1/5 molar ratios. The results indicate that the amylose is more easily degraded to small fragments than amylopectin during the oxidation process. An enzymatic starch analysis method was applied on the oxidized samples. This method was found suitable for estimating the total content of introduced keto and carboxylic groups into the modified product.
Water treatment for thermal recovery (1965)

The economic success or failure in a steam drive may depend on the cost of repair of an oil-field steam generator, and on the number of days of downtime needed to make those repairs. One way to keep the steamers going is to make sure the feedwater is not harmful to the system. Some considerations regarding water-treating are as follows: (1) Steam-generator corrosion control should be directed toward reduction of damage to the protective magnetite layer that forms during normal operation; (2) oxygen and sulfides should be eliminated, the feedwater should be carefully filtered and softened, and the scale-forming tendencies of the feedwater should be monitored by use of coupons as the steam discharge point, for even small amounts of scale will decrease heat-transfer efficiency and increase operating costs; and (3) alkalinity, highly soluble dissolved salts, and pH should not be troublesome within reasonable limits. (15 refs.)
Electrodeless Plasma Thruster Design (2005)

The Elwing Company has designed, built and tested various configurations of its electrodeless plasma thruster technology. The new concept of ponderomotive accelerator has been created to overcome fundamental plasma density limitations in order to reach high thrust density. Among the many possible ways to create the electromagnetic field structures required to produce the ponderomotive force field, the work described in this article focus on the rationale behind the design actually retained for the first prototypes. The impact of the magnetic field geometry on the ionization stage and on the thrust vectoring stage is specifically discussed. The specific design modifications for use at low power (below 1kW) are also exposed.
Linear microwave amplification with Gunn oscillators (1967)

Linear microwave amplifiers with continuous power outputs of 100 mW have been constructed utilizing the frequency-independent negative conductance observed externally in Gunn oscillators. This negative conductance is exhibited only in samples containing propagating dipole layers, in other words, <tex xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">n_{0} . L</tex> must be larger than 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">12</sup> cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">-2</sup> for n-GaAs. The output power obtainable from this amplifier is substantially larger than that from a subcritically doped GaAs amplifier ( <tex xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">n_{0} . L < 10^{12}</tex> cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">-2</sup> ) because <tex xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">n_{0} . L</tex> can be increased. Power output and efficiency are discussed in terms of n <inf xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</inf> and <tex xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">L</tex> . The upper-frequency limit for amplification is determined by the time the domain takes to readjust itself after a change of external voltage which leads to an upper limit for the <tex xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">f. L</tex> product (about 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">8</sup> cm/s). The essential feature of the amplifier circuit is to provide both a short circuit at the Gunn oscillation frequency and a broadband circuit at the signal frequency. An average gain of 3 dB was exhibited from 5.5 GHz to 6.5 GHz. Gain compression of 1 dB occurred at 60 mW output power with 9 dB gain, while the noise figure was about 19 dB.
Systemic Corticosteroids Decrease the Effectiveness of Talc Pleurodesis (1998)

Corticosteroids can inhibit the inflammatory process and the formation of fibrosis. The purpose of this study was to determine whether the concurrent use of steroids at the time of talc-slurry pleurodesis would influence the development of the pleurodesis. One group of rabbits received an intrapleural injection of talc (400 mg/kg) and an intramuscular injection of triamcinolone (0.8 mg/kg) 1 d before talc instillation and weekly thereafter, whereas a control group received only talc. Ten rabbits in each group were killed at 6 h and at 1, 2, 4, 7, 14, and 28 d after instillation. The mean volume of pleural fluid was significantly lower in the group receiving corticosteroids at 6 h through 4 d after talc slurry than in the other groups. The degree of pleural adhesion was significantly smaller in the group receiving corticosteroids from Day 2 through Day 28. At Day 28, all 10 rabbits that received talc only had a pleurodesis score of 3 or 4, whereas only four of the 10 rabbits that also received steroids had a pleurodesis score of 3 or 4. This study shows that the use of corticosteroids at the time of talc-slurry pleurodesis markedly decreases the inflammatory reaction to the talc, and essentially prevents a pleurodesis from developing.
Trust Region Newton Method for Logistic Regression (2008)

Large-scale logistic regression arises in many applications such as document classification and natural language processing. In this paper, we apply a trust region Newton method to maximize the log-likelihood of the logistic regression model. The proposed method uses only approximate Newton steps in the beginning, but achieves fast convergence in the end. Experiments show that it is faster than the commonly used quasi Newton approach for logistic regression. We also extend the proposed method to large-scale L2-loss linear support vector machines (SVM).
ChemInform Abstract: Synthesis of a Thiophene Analogue (VII) of Confusarine. (2009)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 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.
Facile Synthesis of Tetrafluorotyrosine and Its Application in pH Triggered Membrane Lysis (2010)

"Smart" peptides that lyse membranes in response to biological stimuli are of considerable interest. Herein, we report a facile synthesis of L-tetrafluorotyrosine (L-f(4)Y) and its utilization as a pH sensing element. The synthetic route affords gram quantities of L-f(4)Y within two days. Incorporation of this unnatural amino acid into magainin 2 gives a peptide that turns on its membrane-lytic activity upon mild acidification.
Near-zone fields behind circular apertures in thick, perfectly conducting screens (1989)

A rigorous electromagnetic theory describing diffraction by a circular aperture in a perfectly conducting screen is used to model the flux and field intensity profiles in the near field behind the screen. In particular, the case of an aperture having a diameter one-fifth that of the wavelength of the radiation being used is considered. The degree of collimation of both the Poynting vector and the electric field intensity profiles of the transmitted beam is observed and its decrease with increasing distance from the screen is investigated. The effect of increasing the thickness of the screen is observed. These results are relevant to the study of near-field microscopy where the sample under investigation is either imaged with a collimated beam or light transmitted through the object is sampled using a probe having an electrically small diameter.