gebhart/patrepeval huggingface dataset:
Pyrazolo[3,4-d]pyrimidine ribonucleosides as anticoccidials. 3. Synthesis and activity of some nucleosides of 4-[(arylalkenyl)thio]pyrazolo[3,4-d]pyrimidines (1983)

Ribonucleosides of 4-(alkylthio)-1H-pyrazolo[3,4-d]pyrimidines have been shown to be useful anticoccidial agents [Krenitsky, T. A.; Rideout, J. L.; Koszalka, G. W.; Inmon, R. B.; Chao, E. Y.; Elion, G. B.; Latter, V. S.; Williams, R. B. J. Med. Chem. 1982, 25, 32. Rideout, J. L.; Krenitsky, T. A.; Elion, G. B. U.S. Patent 4299 283, 1981]. In that study, the unsaturated 4-allylthio and 4-crotylthio derivatives (19 and 20) were shown to be more active in vivo against Eimeria tenella than their saturated congeners; therefore, some unsaturated (arylalkyl)thio derivatives were synthesized and investigated as anticoccidial agents. The novel compounds in this study (2 to 18) were prepared by the alkylation of 4-mercapto-1-beta-D-ribofuranosyl-1H-pyrazolo[3,4-d]pyrimidine (1), which was prepared by an enzymatic method. The (E)-4-cinnamylthio derivative (2) and the 5'-monophosphate (18) were the most active compounds against E. tenella in vivo. None of the analogues with substituents in the aryl moiety (3 to 13) was more active than 2 in vivo. The geometry about the double bond was important, since the (Z)-4-cinnamylthio derivative (14) was inactive both in vitro and in vivo. The 4-(3-phenylpropynyl)thio and 4-(5-phenyl-2,4-pentadienyl)thio derivatives (15 and 16) were at least as active as 2 in vitro; however, they were less active than 2 in vivo. Compound 2 was effective in vivo against E. tenella, E. necatrix, E. maxima, and E. brunetti; these species of Eimeria were controlled when 2 was given in the diet at levels upt to 100 ppm. Infections in vivo due to E. acervulina were controlled by 2 only at about 800 ppm. The broad spectrum of anticoccidial activity shown by 2 represents a significant improvement over the activities reported for related compounds [Krenitsky, T. A.; Rideout, J. L.; Koszalka, G. W.; Inmon, R. B.; Chao, E. Y.; Elion, G. B.; Latter, V. S.; Williams, R. B. J. Med. Chem. 1982, 25, 32].
Vibration proofing structure of pedal for vehicle (1994)

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 Yoshimasa Kataumi, Yoshinobu Kondo; Vibration proofing structure of pedal for vehicle. J. Acoust. Soc. Am. 1 September 1994; 96 (3): 1945. https://doi.org/10.1121/1.411320 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 ContentAcoustical Society of AmericaThe Journal of the Acoustical Society of America Search Advanced Search |Citation Search
Total Synthesis of Thailanstatin A (2016)

The total synthesis of the spliceosome inhibitor thailanstatin A has been achieved in a longest linear sequence of nine steps from readily available starting materials. A key feature of the developed synthetic strategy is the implementation of a unique, biomimetic asymmetric intramolecular oxa-Michael reaction/hydrogenation sequence that allows diastereodivergent access to highly functionalized tetrahydropyrans, which can be used for the synthesis of designed analogues of this bioactive molecule.
A mathematical model to optimize the drain phase in gravity-based peritoneal dialysis systems. (2010)

Use of patient-specific drain-phase parameters has previously been suggested to improve peritoneal dialysis (PD) adequacy. Improving management of the drain period may also help to minimize intraperitoneal volume (IPV). A typical gravity-based drain profile consists of a relatively constant initial fast-flow period, followed by a transition period and a decaying slow-flow period. That profile was modeled using the equation VD(t) = (V(D0) - Q(MAX) x t) xphi + (V(D0) x e(-alphat)) x (1 - phi), where V(D)(t) is the time-dependent dialysate volume; V(D0), the dialysate volume at the start of the drain; Q(MAX), the maximum drain flow rate; alpha, the exponential drain constant; and phi, the unit step function with respect to the flow transition. We simulated the effects of the assumed patient-specific maximum drain flow (Q(MAX)) and transition volume (psi), and the peritoneal volume percentage when transition occurs,for fixed device-specific drain parameters. Average patient transport parameters were assumed during 5-exchange therapy with 10 L of PD solution. Changes in therapy performance strongly depended on the drain parameters. Comparing 400 mL/85% with 200 mL/65% (Q(MAX/psi), drain time (7.5 min vs. 13.5 min) and IPV (2769 mL vs. 2355 mL) increased when the initial drain flow was low and the transition quick. Ultrafiltration and solute clearances remained relatively similar. Such differences were augmented up to a drain time of 22 minutes and an IPV of more than 3 L when Q(MAX) was 100 mL/min. The ability to model individual drain conditions together with water and solute transport may help to prevent patient discomfort with gravity-based PD. However, it is essential to note that practical difficulties such as displaced catheters and obstructed flow paths cause variability in drain characteristics even for the same patient, limiting the clinical applicability of this model.
Tryptamine-Gallic Acid Hybrid Prevents Non-steroidal Anti-inflammatory Drug-induced Gastropathy (2011)

We have investigated the gastroprotective effect of SEGA (3a), a newly synthesized tryptamine-gallic acid hybrid molecule against non-steroidal anti-inflammatory drug (NSAID)-induced gastropathy with mechanistic details. SEGA (3a) prevents indomethacin (NSAID)-induced mitochondrial oxidative stress (MOS) and dysfunctions in gastric mucosal cells, which play a pathogenic role in inducing gastropathy. SEGA (3a) offers this mitoprotective effect by scavenging of mitochondrial superoxide anion (O(2)(·-)) and intramitochondrial free iron released as a result of MOS. SEGA (3a) in vivo blocks indomethacin-mediated MOS, as is evident from the inhibition of indomethacin-induced mitochondrial protein carbonyl formation, lipid peroxidation, and thiol depletion. SEGA (3a) corrects indomethacin-mediated mitochondrial dysfunction in vivo by restoring defective electron transport chain function, collapse of transmembrane potential, and loss of dehydrogenase activity. SEGA (3a) not only corrects mitochondrial dysfunction but also inhibits the activation of the mitochondrial pathway of apoptosis by indomethacin. SEGA (3a) inhibits indomethacin-induced down-regulation of bcl-2 and up-regulation of bax genes in gastric mucosa. SEGA (3a) also inhibits indometacin-induced activation of caspase-9 and caspase-3 in gastric mucosa. Besides the gastroprotective effect against NSAID, SEGA (3a) also expedites the healing of already damaged gastric mucosa. Radiolabeled ((99m)Tc-labeled SEGA (3a)) tracer studies confirm that SEGA (3a) enters into mitochondria of gastric mucosal cell in vivo, and it is quite stable in serum. Thus, SEGA (3a) bears an immense potential to be a novel gastroprotective agent against NSAID-induced gastropathy.
Synthesis and Receptor Affinity of Polysubstituted Adenosines (1999)

In a search for potent and selective adenosine agonists it has been found that 2-hexynyladenosine-5'-N-ethyluronamide (HENECA) displays high affinity at rat A2A receptor combined with a good A2A vs A1 selectivity. The finding that HENECA shows good affinity also for A3 receptors prompted us to investigate the effect of various substituents in different positions of this molecule.
Experimental Evidence for the Quasi-“Living” Nature of the Grignard Metathesis Method for the Synthesis of Regioregular Poly(3-alkylthiophenes) (2005)

The Grignard metathesis (GRIM) polymerization of 3-alkylthiophenes proceeds by a quasi-“living” chain growth mechanism, not by a step growth process. Kinetic studies of the Grignard metathesis polymerization of 2,5-dibromo-3-alkylthiophenes showed that the molecular weight of poly(3-alkylthiophenes) is a function of the molar ratio of the monomer to nickel initiator, and conducting polymers with predetermined molecular weights and relatively narrow molecular weight distributions (PDIs = 1.2−1.5) can be made. Sequential monomer addition resulted in new block copolymers containing different poly(3-alkylthiophene) segments.
Iterative Learning Control For Periodic Disturbances in Twin-Roll Strip Casting with Measurement Delay (2018)

We consider the problem of periodic disturbances in the thickness profile of a strip produced using the twin-roll casting process. In twin-roll casting, a strip is produced by pouring molten metal on the surface of two casting rolls that simultaneously cool and compress the strip as they rotate. This rotational motion can produce periodic disturbances in the thickness profile due to angular variations in the shape and thermodynamic characteristics of the rolls. Compensating for these disturbances is further complicated by the fact that there exist large measurement delays between the initial casting and the thickness profile measurement. This paper explores the use of an iterative learning control (ILC) algorithm to reduce the influence of these disturbances on a per-revolution basis. Further consideration is given to managing the measurement delay within the ILC framework. Simulation results show that the proposed controller is able to minimize the effect of the periodic disturbance on the strip thickness profile.
Development of a Novel Artificial Urinary Sphincter: A Versatile Automated Device (2010)

Management of male severe stress urinary incontinence is currently achieved by the treatment of choice: an artificial urinary sphincter (AUS). This implantable system is designed to exert a constant circumferential force around the urethra. Although continence is totally or partially recovered in most of the patients, this method has some significant drawbacks. Besides the difficulty and discomfort of using the device, the revision rate caused by constant urethral compression, leading to urethral injuries, remains high. We present in this study a new AUS concept, with an ergonomic control, providing a lower exerted pressure on the urethral tissues and improving the continence efficiency. In fact, the implant includes a system which automatically detects circumstances involving high-intravesical pressure and adapts the occlusive pressure accordingly. The device was evaluated using isolated goat urethra, and then, in vivo. Recorded data of 16 human subjects performing different daily exercises were used to assess the detection algorithms. It is shown that occlusive pressure can be controlled by the implant with an accuracy of 1 <formula formulatype="inline" xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"><tex Notation="TeX">$\hbox{cm H}_{2}\hbox{O}$</tex> </formula> (98 Pa). Acceptable detection performance of seven of the eight targeted activities was observed.
Celp Coding Based On Signal Classification Using The Dyadic Wavelet Transform (1996)

Publication in the conference proceedings of EUSIPCO, Trieste, Italy, 1996
Optimal Construction of Regenerating Code through Rate-matching in Hostile Networks (2015)

Regenerating code is a class of code very suitable for distributed storage systems, which can maintain optimal bandwidth and storage space. Two types of important regenerating code have been constructed: the minimum storage regeneration (MSR) code and the minimum bandwidth regeneration (MBR) code. However, in hostile networks where adversaries can compromise storage nodes, the storage capacity of the network can be significantly affected. In this paper, we propose two optimal constructions of regenerating codes through rate-matching that can combat against this kind of adversaries in hostile networks: 2-layer rate-matched regenerating code and $m$-layer rate-matched regenerating code. For the 2-layer code, we can achieve the optimal storage efficiency for given system requirements. Our comprehensive analysis shows that our code can detect and correct malicious nodes with higher storage efficiency compared to the universally resilient regenerating code which is a straightforward extension of regenerating code with error detection and correction capability. Then we propose the $m$-layer code by extending the 2-layer code and achieve the optimal error correction efficiency by matching the code rate of each layer's regenerating code. We also demonstrate that the optimized parameter can achieve the maximum storage capacity under the same constraint. Compared to the universally resilient regenerating code, our code can achieve much higher error correction efficiency.
Enzyme-Linked Immunosorbent Assay Based on Soluble Promastigote Antigen Detects Immunoglobulin M (IgM) and IgG Antibodies in Sera from Cases of Visceral and Cutaneous Leishmaniasis (2002)

Leishmaniasis causes significant morbidity and mortality in areas where it is endemic. In areas where it is nonendemic, global travel and increased incidence of the disease in human immunodeficiency virus and intravenous-drug user populations are also causes for concern. The unavailability of rapid and reliable tests for diagnosis of the various leishmaniases makes patient management difficult. We have developed an enzyme-linked immunosorbent assay (ELISA) that can detect immunoglobulin M (IgM) and IgG antibodies in patients with visceral and cutaneous leishmaniasis. These practical assays are based on soluble antigens from promastigotes cultivated in a protein-free medium. In preliminary studies, 129 visceral (Brazil, Italy, North Africa, and Nepal) and 143 cutaneous (Brazil) leishmaniasis patients with controls were tested. Overall, the tests showed a sensitivity of 95.1%. In addition, the ELISA correctly identified 42 sera from Brazilian dogs with canine leishmaniasis and 10 healthy controls. Serological tests for the various clinical manifestations of leishmaniasis could be useful epidemiological and patient management tools in populations of areas of endemicity and nonendemicity.
HFR1, a phytochrome A‐signalling component, acts in a separate pathway from HY5, downstream of COP1 in <i>Arabidopsis thaliana</i> (2002)

HFR1, a basic helix-loop-helix protein, is known to be required for a subset of phytochrome A (phyA)-dependent photoresponses. To investigate the role of HFR1 in light signalling, we have examined the genetic interaction between HFR1 and HY5, a positive regulator of light signalling, and COP1, a repressor of photomorphogenesis. Double mutant analysis suggests that HFR1 mediates phyA-dependent inhibition of hypocotyl elongation independently of HY5. HFR1 was shown to be necessary for a subset of cop1-triggered photomorphogenic phenotypes in the dark, including inhibition of hypocotyl elongation, gravitropic hypocotyl growth, and expression of the light-inducible genes CAB and RBCS. Phenotypic analysis of the triple mutant cop1hy5hfr1 indicated that both HFR1 and HY5 are required for cop1-mediated photomorphogenic seedling development in darkness, consistent with their additive roles in phyA-dependent signalling. Taken together, these results suggest that HFR1 might act downstream of COP1, in a separate pathway from HY5, to mediate photomorphogenesis in Arabidopsis.
Agile beam steering using phased-arraylike binary optics (1994)

A method is demonstrated for two-dimensional steering of a laser beam by way of the mechanical translation of two phased-arraylike binary optics elements. The elements are translated over a 320-pum distance, resulting in the steering of a green He-Ne laser (λ = 0.543 µm) over a 6-deg field of view. Both theoretical development and experimental verification are presented.
Panache: a parallel file system cache for global file access (2010)

Cloud computing promises large-scale and seamless access to vast quantities of data across the globe. Applications will demand the reliability, consistency, and performance of a traditional cluster file system regardless of the physical distance between data centers.Panache is a scalable, high-performance, clustered file system cache for parallel data-intensive applications that require wide area file access. Panache is the first file system cache to exploit parallelism in every aspect of its design--parallel applications can access and update the cache from multiple nodes while data and metadata is pulled into and pushed out of the cache in parallel. Data is cached and updated using pNFS, which performs parallel I/O between clients and servers, eliminating the single-server bottleneck of vanilla client-server file access protocols. Furthermore, Panache shields applications from fluctuating WAN latencies and outages and is easy to deploy as it relies on open standards for high-performance file serving and does not require any proprietary hardware or software to be installed at the remote cluster.In this paper, we present the overall design and implementation of Panache and evaluate its key features with multiple workloads across local and wide area networks.
Electroporation-Induced Electrosensitization (2011)

For varied experimental conditions, EPs triggered a delayed and gradual sensitization to EPs. When a portion of a multi-pulse exposure was delivered to already sensitized cells, the overall effect markedly increased. Because of the sensitization, the lethality in EP-treated cells could be increased from 0 to 90% simply by increasing the exposure duration, or the exposure dose could be reduced twofold without reducing the effect. Many applications of electroporation can benefit from accounting for sensitization, by organizing the exposure either to maximize sensitization (e.g., for sterilization) or, for other applications, to completely or partially avoid it. In particular, harmful side effects of electroporation-based therapies (electrochemotherapy, gene therapies, tumor ablation) include convulsions, pain, heart fibrillation, and thermal damage. Sensitization can potentially be employed to reduce these side effects while preserving or increasing therapeutic efficiency.
Ligand-accelerated enantioselective methylene C(sp <sup>3</sup> )–H bond activation (2016)

Effective differentiation of prochiral carbon-hydrogen (C-H) bonds on a single methylene carbon via asymmetric metal insertion remains a challenge. Here, we report the discovery of chiral acetyl-protected aminoethyl quinoline ligands that enable asymmetric palladium insertion into prochiral C-H bonds on a single methylene carbon center. We apply these palladium complexes to catalytic enantioselective functionalization of β-methylene C-H bonds in aliphatic amides. Using bidentate ligands to accelerate C-H activation of otherwise unreactive monodentate substrates is crucial for outcompeting the background reaction driven by substrate-directed cyclopalladation, thereby avoiding erosion of enantioselectivity. The potential of ligand acceleration in C-H activation is also demonstrated by enantioselective β-C-H arylation of simple carboxylic acids without installing directing groups.
"Edge illumination" in X-ray Phase Contrast Imaging (2012)

In the late '90s, the concept of "edge illumination" was developed at ELETTRA in Italy as an alternative method to increase the phase sensitivity of an imaging system. The main idea was to be able to reproduce the fine angular selection of "analyzer" crystals without actually using a crystal, as this would allow employing the method with divergent and polychromatic (i.e. conventional) x-ray sources. It was observed that this could be achieved by illuminating only the edges of the detector pixels, and that the method's sensitivity could be progressively increased by illuminating smaller pixel fractions closer to its physical edge. A few years later the idea was adapted for use with a conventional source by means of two sets of x-ray masks ("coded aperture" masks), which enabled obtaining the same effect for each row (or column) of pixels of an area detector illuminated by a cone beam. This article reviews the method and presents recent examples of application.
Single-element laser beam shaper for uniform flat-top profiles (2003)

A novel design method is presented for a simple laser beam shaper. Unlike earlier reports and designs based on the 2-element model, we prove it is possible to convert a laser beam from a non-uniform profile to a uniform flat-top distribution with one single aspherical lens.
TAR1, A Human Anti-p53 Single-Chain Antibody, Restores Tumor Suppressor Function to Mutant p53 Variants (2010)

The tumor suppressor gene p53 is mutated in more than half of human tumors. One important characteristic of p53 mutants is their accumulation in the nucleus of cancer cells. Thus, reactivation of mutant p53 proteins may trigger massive apoptosis in tumor cells. Pharmacologic methods are currently under development to induce mutant p53 proteins to resume their wild-type function. We have identified a human single-chain Fv fragment, designated as transcriptional transactivation and apoptosis restoring (TAR1), which specifically and with high affinity binds to mutant p53 and restores its wild-type active conformation. Binding of TAR1 to mutant p53 induced transcriptional transactivation of p53 target genes and down-regulation of mutant p53 transcriptional target genes. TAR1 treatment induced apoptosis in a variety of cell lines endogenously expressing p53 carrying different point mutations DNA contact or structural p53 mutants. Moreover, in an animal model of mice carrying human xenografts, TAR1 induced tumor regression with no apparent deleterious side effects. Thus, it may be considered as a potential candidate for anticancer treatment, targeting tumors with mutant p53.
Increased Efficacy and Safety in the Treatment of Experimental Liver Cancer with a Novel Adenovirus-Alphavirus Hybrid Vector (2006)

An improved viral vector for cancer gene therapy should be capable of infecting tumors with high efficiency, inducing specific and high-level expression of transgene in the tumor and selectively destroying tumor cells. In the design of such a vector to treat hepatocellular carcinoma, we took advantage of (a) the high infectivity of adenoviruses for hepatic cells, (b) the high level of protein expression and proapoptotic properties that characterize Semliki Forest virus (SFV) replicon, and (c) tumor selectivity provided by alpha-fetoprotein (AFP) promoter. We constructed a hybrid viral vector composed of a helper-dependent adenovirus containing an SFV replicon under the transcriptional control of AFP promoter and a transgene driven by SFV subgenomic promoter. Hybrid vectors containing murine interleukin-12 (mIL-12) genes or reporter gene LacZ showed very specific and high-level expression of transgenes in AFP-expressing hepatocellular carcinoma cells, both in vitro and in an in vivo hepatocellular carcinoma animal model. Infected hepatocellular carcinoma cells were selectively eliminated due to the induction of apoptosis by SFV replication. In a rat orthotopic liver tumor model, treatment of established tumors with a hybrid vector carrying mIL-12 gene resulted in strong antitumoral activity without accompanying toxicity. This new type of hybrid vectors may provide a potent and safe tool for cancer gene therapy.