gebhart/patrepeval huggingface dataset:
1,5‐naphthyridines. Synthesis of 7‐chloro‐4‐(4‐diethylamino‐1‐methylbutylamino)‐2‐methoxy‐1,5‐naphthyridine and related compounds (1970)

Abstract The synthesis of 7‐chloro‐4‐(4‐diethylamino‐1‐methylbutylamino)‐2‐methoxy‐1,5‐naphthyridine, a compound which incorporates the structure of both chloroquine (a schizontocidal drug) and pamaquine (a gametocytocidal drug), has been carried out. In addition, two structurally related derivatives, the, “5‐azachloroquine” and the “5‐azapamaquine,” have also been obtained by multi‐step syntheses. “5‐Azachloroquine” possesses good antimalarial activity against Plasmodium berghei. The compound was also found to be less toxic than the known 4‐aminoquinoline and 8‐aminoquinoline antimalarial drugs.
Microwave‐assisted RCM for the synthesis of carbocyclic peptides (2007)

Microwave irradiation dramatically improves the efficiency of ring closing metathesis (RCM) reactions of resin-attached peptides and the technology is illustrated by the highly selective synthesis of dicarba analogues of alpha-conotoxin IMI.
29; RECOVERY OF RIGHT VENTRICULAR FUNCTION AFTER SEVERE HEMORRHAGIC SHOCK-RESUSCITATION USING EXTRACORPOREAL ASSISTED CIRCULATION (1994)

Dan, ; Meyer, M.; Michael, ; Jessen, E.; Barak, Chen; Robert, ; Chao, Y.; Lee, C. Young Author Information
The Cycloaddition Strategy for the Synthesis of Natural Products Containing Carbocyclic Seven‐Membered Rings (2006)

Highly substituted carbocyclic seven-membered rings are frequently found in natural products and their synthesis represents a significant challenge to the synthetic chemist. Direct intramolecular cyclization of these systems often proves difficult and this fact has catalyzed the development of a variety of strategies based on a convergent intermolecular cycloaddition strategy. This concept article discusses the major cycloaddition approaches utilized to access these types of structures and primarily focuses on examples employed in the synthesis of natural products.
The Effect of Aldosterone Antagonists for Ventricular Arrhythmia: A Meta‐Analysis (2010)

The additional administration of AAs in patients with HF or coronary artery disease shows a benefit in reducing the risk of SCD and may also be effective for reducing episodes of ventricular premature complexes and ventricular tachycardia.
Ion Recognition at the Interface of Self-Assembled Monolayers (SAMs) of Bis-Thioctic Ester Derivatives of Oligo(ethyleneglycols) (2000)

Self-assembled monolayers (SAMs) of bis-thioctic ester derivatives of oligoethylene glycols were prepared. When the number of (−CH2−CH2−O−)n units in these podands was either five or six, the corresponding SAMs showed ion binding properties and selectivities similar to those exhibited by 15-crown-5 or 18-crown-6 in aqueous solution, respectively. Impedance data for the SAMs as a function of metal ion concentrations were fitted by using a Langmuir isotherm to determine the association constants (Ka) with the different ions. The SAM derived from the n=5 compound is selective for Na+ while that with n=6 is selective for K+. Results presented here confirm the formation of ion recognition domains during self-assembly of acyclic polyethylene glycol derivatives on gold surfaces; this suggests that surface-confined pseudocrown ether structures are formed.
On Optimal SINR-Based Scheduling in Multihop Wireless Networks (2010)

In this paper, we revisit the problem of determining the minimum-length schedule that satisfies certain traffic demands in a wireless network. Traditional approaches for the determination of minimum-length schedules are based on a collision channel model, in which neighboring transmissions cause destructive interference if and only if they are within the “interference region” of the receiving nodes. By contrast, we adopt here a more realistic model for the physical layer by requiring that a threshold be exceeded by the signal-to-interference-plus-noise ratio (SINR) for a transmission to be successful. We present a novel formulation of the problem that incorporates various power and rate adaptation schemes while seamlessly integrating the generation of “matchings” (i.e., sets of links that can be activated simultaneously) by taking into consideration the SINR constraints at the receivers. For the formulated problem, we propose a column-generation-based solution method and show that it theoretically converges to a globally optimal solution, with a potential advantage of not having to enumerate all the feasible matchings a priori. We also discuss the influence of power control, spatial reuse, and variable transmission rates on network performance. Furthermore, we include aspects of the routing problem and provide computational results for our proposed column-generation-based solution procedure.
Glucocorticoid inhibition of c-myc, c-myb, and c-Ki-ras expression in a mouse lymphoma cell line. (1986)

Glucocorticoid hormone treatment of certain T-cell-derived lymphomas and leukemias and of immature thymocytes results in cell death. Furthermore, glucocorticoid-mediated killing of S49 mouse lymphoma cells appears to involve the control of the cell cycle; i.e., S49 cells treated with glucocorticoids are arrested in G1 of the cell cycle when events controlling cell proliferation occur. The protooncogenes, c-myc, c-myb, and c-Ki-ras may be involved in cell cycle regulation and proliferation state in both normal and neoplastic cells. We report here that the steady state mRNA levels of c-myc, c-myb, and c-Ki-ras in S49 cells are dramatically and rapidly decreased after glucocorticoid treatment. Minimal expression is observed after 9 h, remaining at a constant low level at 11 h. Flow cytometry reveals no significant alteration in the cell cycle distribution of S49 cells up to 12 h after treatment. These findings suggest that glucocorticoids suppress the expression of these protooncogenes and that this may be the mechanism whereby glucocorticoids inhibit cell cycle progression in T-lymphoid cell lines.
Treatment of Malignant Primary Vasodepressive Neurocardiogenic Syncope with a Rate Responsive Pacemaker Driven by Heart Contractility (1998)

In a 41-year-old man suffering from frequent syncope, the tilt test reproducibly induced a primary vasodepressive neurocardiogenic syncope. Pharmacotherapy either failed to prevent the syncope induced at the tilt test or was poorly tolerated. In the minutes preceding the syncope, a dramatic increase in heart contractility was sensed by a microaccelerometer located at the tip of a right ventricular pacing electrode. When the tilt test was repeated with the pacemaker programmed in the DDDR mode, high rate dual chamber pacing occurred during the tilt phase and prevented the syncope. Three months after implantation, the patient remains totally symptom free.
Leishmaniasis Worldwide and Global Estimates of Its Incidence (2012)

As part of a World Health Organization-led effort to update the empirical evidence base for the leishmaniases, national experts provided leishmaniasis case data for the last 5 years and information regarding treatment and control in their respective countries and a comprehensive literature review was conducted covering publications on leishmaniasis in 98 countries and three territories (see 'Leishmaniasis Country Profiles Text S1, S2, S3, S4, S5, S6, S7, S8, S9, S10, S11, S12, S13, S14, S15, S16, S17, S18, S19, S20, S21, S22, S23, S24, S25, S26, S27, S28, S29, S30, S31, S32, S33, S34, S35, S36, S37, S38, S39, S40, S41, S42, S43, S44, S45, S46, S47, S48, S49, S50, S51, S52, S53, S54, S55, S56, S57, S58, S59, S60, S61, S62, S63, S64, S65, S66, S67, S68, S69, S70, S71, S72, S73, S74, S75, S76, S77, S78, S79, S80, S81, S82, S83, S84, S85, S86, S87, S88, S89, S90, S91, S92, S93, S94, S95, S96, S97, S98, S99, S100, S101'). Additional information was collated during meetings conducted at WHO regional level between 2007 and 2011. Two questionnaires regarding epidemiology and drug access were completed by experts and national program managers. Visceral and cutaneous leishmaniasis incidence ranges were estimated by country and epidemiological region based on reported incidence, underreporting rates if available, and the judgment of national and international experts. Based on these estimates, approximately 0.2 to 0.4 cases and 0.7 to 1.2 million VL and CL cases, respectively, occur each year. More than 90% of global VL cases occur in six countries: India, Bangladesh, Sudan, South Sudan, Ethiopia and Brazil. Cutaneous leishmaniasis is more widely distributed, with about one-third of cases occurring in each of three epidemiological regions, the Americas, the Mediterranean basin, and western Asia from the Middle East to Central Asia. The ten countries with the highest estimated case counts, Afghanistan, Algeria, Colombia, Brazil, Iran, Syria, Ethiopia, North Sudan, Costa Rica and Peru, together account for 70 to 75% of global estimated CL incidence. Mortality data were extremely sparse and generally represent hospital-based deaths only. Using an overall case-fatality rate of 10%, we reach a tentative estimate of 20,000 to 40,000 leishmaniasis deaths per year. Although the information is very poor in a number of countries, this is the first in-depth exercise to better estimate the real impact of leishmaniasis. These data should help to define control strategies and reinforce leishmaniasis advocacy.
Performance Model for Orthogonal Sub Channel in Noise-Limited Environment (2010)

Orthogonal Sub Channel (OSC) is a voice enhancement for the GSM evolution. It allows in principle a double capacity with the same hardware compared to the previous GSM Half Rate (HR) mode. This paper investigates the effects of OSC on the radio performance as function of the OSC capable handset penetration compared to the GSM HR mode. A set of test cases was carried out in GSM network in order to evaluate the radio performance of OSC in terms of the carrier per noise level. The tests were performed in noise-limited indoor environment, and the quality and received power level distributions were analyzed. As a main achievement, a generic model for estimating the effect of OSC on the GSM radio performance was developed. The model is based on the network statistics and performance indicators of GSM.
THE CRYSTAL STRUCTURE OF AN ALL-RNA HAMMERHEAD RIBOZYME: A PROPOSED MECHANISM FOR RNA CATALYTIC CLEAVAGE (1995)

We have solved the crystal structure of an all-RNA hammerhead ribozyme by isomorphous replacement which contains a single 2'-O-methyl-cytosine at the active site to prevent cleavage. We describe the hammerhead RNA structure from a point of view which shows how the structural elements are disposed to bring the active site nucleotide into the catalytic pocket of the ribozyme. Five potential Mg(II) binding sites can be identified in the hammerhead RNA electron density maps. Of these, one is a newly identified metal site positioned near the ribozyme catalytic pocket, and another site corresponds to a Mn(II) site identified in the previous hammerhead RNA structure. We propose a mechanism for RNA catalytic cleavage on the basis of this new metal-binding site, as well as upon comparisons between the catalytic pocket of the hammerhead RNA and the metal-binding sites in the structurally homologous uridine turn of the anticodon loop in tRNAPhe.
Intermolecular Coupling of Alkenes to Heterocycles via C−H Bond Activation (2004)

The intermolecular coupling of unactivated alkenes to a range of heterocycles using a Rh(I) catalyst was investigated. A variety of functional groups were incorporated into the alkene, including esters, nitriles, acetals, and phthalimide. Furthermore, the heterocycle tolerated substitution with both electron-rich and electron-deficient groups. The intermolecular coupling became possible after it was discovered that weak acids dramatically increase the rate of both the inter- and intramolecular reactions. An extensive optimization of additives was performed, and HCl.PCy(3) (Cy = cyclohexyl) and HCl.P-t-Bu(2)Et were in general found to be the best additives for the reaction.
Glycine: A Possible Role in Lithium’s Action and Affective Illness (1983)

In addition to its incorporation into proteins, glycine functions as both a regulator of one-carbon metabolism and as an inhibitory neurotransmitter. Clinical recognition of the hyperglycinemias and reported elevations of erythrocyte glycine concentrations in patients with bipolar disorders have implicated this amino acid in the etiopathology of some neuropsychiatric disorders. Moreover, chronic lithium administration, an almost specific intervention for the treatment and prophylaxis of bipolar disorders, has been shown to induce elevations in brain and erythrocyte glycine levels. In view of glycine's complex metabolic interrelationships and neurotransmitter function, additional research exploring its possible role in either affective illness or lithium's action is indicated.
Information transfer in disordered media by broadband time-reversal: stability, resolution and capacity (2006)

We analyse rigorously the time reversal of a multiple-input-multiple-output system in a strongly fluctuating disordered medium described by the stochastic Schrödinger equation with a random potential under the sub-Gaussian assumption. We prove that in a broadband limit the conditions for stable super-resolution are the packing condition such that the spacing among the N transmitters and M receivers be more than the coherence length ℓc and the consecutive symbols in the datum streams are separated by more than the inverse of the bandwidth B−1 and the multiplexing (or stability) condition such that the number of the degrees of freedom per unit time at the transmitters (∼NB) be much larger than the number of the degrees of freedom (∼MC) per unit time in the ensemble of intended messages. Here C is the number of symbols per unit time in the datum streams intended for each receiver. When the two conditions are met, all receivers simultaneously receive streams of statistically stable, sharply focused signals intended for them, free of fading and interference. We show that an O(P/ν) information rate P/ν can be achieved with statistical stability under the condition N ≫ M ≫ P/(ν B) where P is the average total power constraint and ν the noise power per unit bandwidth. The packing condition then implies that in the optimal transfer regime where γ is the Fresnel number, βc the coherence bandwidth and d the transverse dimension. Our results should be valid for diffusive waves with βc = Thouless frequency. Therefore, under the ideal packing and multiplexing conditions time reversal communications result in a high signal-to-interference ratio and low probability of intercept and is an effective means for achieving the information capacity of disordered media in the presence of multiple users.
Thermomechanical behavior of ceramic ball grid array based on experiments and FEM simulations (2002)

In this paper, we have performed 2D finite element simulations on CBGA components assembled on FR4 card in order to evaluate the highest stressed regions of the solder joint. The maximum cumulative strain energy has been calculated as a function of the thermal cycling characteristics and of the package size to evaluate the fatigue of the solder joints. Accelerated ageing tests (0/spl deg/C to 100/spl deg/C) have been performed on CBGA samples to validate such a global approach. The analysis of the degradation have been performed using direct observation with SEM and also a specific procedure of acoustic imaging allowing the detection of defects located on the inner balls. From the previous FEM simulation results and the experimental data under thermal cycling, we propose a global interpretation, based on general mechanical laws, of the thermomechanical behavior of the CBGA solder joints under thermal cycling. Conclusions about the evolution of the CBGA assemblies criticity with both package size and ball number increase are deduced from this study.
Use of targetrons to disrupt essential and nonessential genes in <i>Staphylococcus aureus</i> reveals temperature sensitivity of Ll.LtrB group II intron splicing (2006)

We show that a targetron based on the Lactococcus lactis Ll.LtrB group II intron can be used for efficient chromosomal gene disruption in the human pathogen Staphylococcus aureus. Targetrons expressed from derivatives of vector pCN37, which uses a cadmium-inducible promoter, or pCN39, a derivative of pCN37 with a temperature-sensitive replicon, gave site-specific disruptants of the hsa and seb genes in 37%-100% of plated colonies without selection. To disrupt hsa, an essential gene, we used a group II intron that integrates in the sense orientation relative to target gene transcription and thus could be removed by RNA splicing, enabling the production of functional HSa protein. We show that because splicing of the Ll.LtrB intron by the intron-encoded protein is temperature-sensitive, this method yields a conditional hsa disruptant that grows at 32 degrees C but not 43 degrees C. The temperature sensitivity of the splicing reaction suggests a general means of obtaining one-step conditional disruptions in any organism. In nature, temperature sensitivity of group II intron splicing could limit the temperature range of an organism containing a group II intron inserted in an essential gene.
Microdose Study of 14C-Acetaminophen With Accelerator Mass Spectrometry to Examine Pharmacokinetics of Parent Drug and Metabolites in Healthy Subjects (2010)

A study of the pharmacokinetics of (14)C-labeled acetaminophen (AAP) was performed in healthy Japanese subjects receiving an oral microdose of the drug. After separation by high-performance liquid chromatography (HPLC), the levels of AAP and its metabolites in the pooled plasma specimens were quantified using accelerator mass spectrometry (AMS). The total body clearance (CL(tot))/bioavailability (F) of AAP was within the variation in the reported values at therapeutic doses, indicating the linearity of AAP pharmacokinetics. AAP-glucuronide (Glu) and AAP-4-O-sulfate satisfied the criteria of safety testing of drug metabolites. AMS could detect AAP-Cys, the active metabolite of AAP conjugated with cysteine, in the urine. Probenecid prolonged the systemic elimination of total radioactivity and caused a marked decrease in AAP-Glu levels in plasma. Probenecid likely inhibited the glucuronidation of AAP and the renal elimination of AAP-4-O-sulfate. Microdosing of (14)C-labeled drug followed by AMS is a powerful tool that can be used in the early phase of drug development for pharmacokinetic analysis of drugs and their metabolites and for detecting the formation of active metabolites in humans.
Circulating miR-210 as a Novel Hypoxia Marker in Pancreatic Cancer (2010)

MicroRNA are small noncoding transcripts involved in many cellular mechanisms, including tumorigenesis. miR-210, in particular, is induced by hypoxia and correlates with adverse outcomes in certain cancers. Because pancreatic adenocarcinomas exhibit extremely hypoxic signatures, we hypothesized that miR-210 may serve as a diagnostic marker for screening or surveillance for pancreatic cancer. Plasma samples were obtained from newly diagnosed pancreatic cancer patients and age-matched noncancer controls. miRNA was extracted directly from plasma and reverse-transcribed to complementary DNA. A known quantity of synthetic Caenorhabditis elegans miR-54 (celmiR-54) was added for normalization. miR-210 and cel-miR-54 were then measured using quantitative reverse transcription polymerase chain reaction. An initial cohort of 11 pancreatic cancer patients and 14 age-matched controls was used as the test set and a second cohort of 11 pancreatic cancer patients and 11 controls was used as the validating set in this study. miR-210 was reliably detected and quantified, with a statistically significant four-fold increase in expression in pancreatic cancer patients compared with normal controls (P < .00004) in the test set. This difference was confirmed in the validation group (P < .018). In summary, circulating miR-210 levels are elevated in pancreatic cancer patients and may potentially serve as a useful biomarker for pancreatic cancer diagnosis.
Predominant Plaque Flora of Tanzanian Children Exposed to High and Low Water Fluoride Concentrations (1979)

The paper provides a detailed bacteriologic description of the predominant flora of supragingival plaque collected from 15 caries-free Tanzanian children exposed to negligible (0.3 ppm) and excessive (3–21 ppm) concentrations of fluoride in the water supply. The three predominant groups of bacteria in all samples were streptococci, veillonellae, and pleomorphic, gram-positive rods, which together accounted for 86.8% (mean) of cultivable flora. Streptococcus mitior was the single most predominant streptococcal species. Streptococcus mutans, mainly of serotype b, was isolated from two thirds of the samples and accounted for 2.3–21.4% of the streptococcal flora. Bacteria, which potentially metabolize lactate, i. e. veillonellae, neisseriae, propionibacteria, arachniae, Bacteroides asaccharolyticus, and Streptococcus jaecalis, comprised almost one half of the total flora (range 9–76%), and may conceivably be responsible for the negligible caries activity, despite the presence of highly acidogenic bacteria. There were no detectable differences in the flora of plaque samples from children exposed to high and low water fluoride concentrations, respectively. Previously observed fluoride-induced differences in the net metabolic product, and contents of extra- and intracellular polysaccharides of plaque, is probably to be explained by a direct interference of fluoride with plaque enzymes.
Transurethral Ultrasonic Uretero-Lithotripsy: A New Technique (1987)

No AccessJournal of Urology1 Jun 1987Transurethral Ultrasonic Uretero-Lithotripsy: A New Technique Christian G. Chaussy, Gerhard J. Fuchs, Robert I. Kahn, Patrick T. Hunter, and Roger Goodfriend Christian G. ChaussyChristian G. Chaussy More articles by this author , Gerhard J. FuchsGerhard J. Fuchs More articles by this author , Robert I. KahnRobert I. Kahn More articles by this author , Patrick T. HunterPatrick T. Hunter More articles by this author , and Roger GoodfriendRoger Goodfriend More articles by this author View All Author Informationhttps://doi.org/10.1016/S0022-5347(17)75374-8AboutPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail "Transurethral Ultrasonic Uretero-Lithotripsy: A New Technique." The Journal of Urology, 137(6), p. 159A © 1987 by The American Urological Association Education and Research, Inc.FiguresReferencesRelatedDetails Volume 137Issue 6June 1987Page: 159A Advertisement Copyright & Permissions© 1987 by The American Urological Association Education and Research, Inc.MetricsAuthor Information Christian G. Chaussy More articles by this author Gerhard J. Fuchs More articles by this author Robert I. Kahn More articles by this author Patrick T. Hunter More articles by this author Roger Goodfriend More articles by this author Expand All Advertisement PDF downloadLoading ...
The FAIN Management Framework: a management approach for active network environments (2003)

The FAIN Management Framework of active and programmable networks is an innovative distributed policy based management framework that copes with the specific management requirements of active networks, dynamically adapting to heterogeneous network technologies and functionalities. Also, it supports a flexible delegation approach with co-existence of different management strategies allowing actors to best customise the management architecture to their business needs. This results in reduction of redundant traffic and information processing, and dynamic fine-grained management tailoring. The paper focuses on how policy-based management is applicable to the active network and how these technologies can merge in an evolutionary management framework. The concepts presented here have been developed within the framework of the FAIN project.