gebhart/patrepeval huggingface dataset:
The total synthesis of alcaligin (1991)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTThe total synthesis of alcaliginR. J. Bergeron, J. S. McManis, P. T. Perumal, and S. E. AlgeeCite this: J. Org. Chem. 1991, 56, 19, 5560–5563Publication Date (Print):September 1, 1991Publication History Published online1 May 2002Published inissue 1 September 1991https://pubs.acs.org/doi/10.1021/jo00019a017https://doi.org/10.1021/jo00019a017research-articleACS PublicationsRequest reuse permissionsArticle Views338Altmetric-Citations28LEARN 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
Decontamination of chemical and biological warfare (CBW) agents using an atmospheric pressure plasma jet (APPJ) (1999)

The atmospheric pressure plasma jet (APPJ) [A. Schütze et al., IEEE Trans. Plasma Sci. 26, 1685 (1998)] is a nonthermal, high pressure, uniform glow plasma discharge that produces a high velocity effluent stream of highly reactive chemical species. The discharge operates on a feedstock gas (e.g., He/O2/H2O), which flows between an outer, grounded, cylindrical electrode and an inner, coaxial electrode powered at 13.56 MHz rf. While passing through the plasma, the feedgas becomes excited, dissociated or ionized by electron impact. Once the gas exits the discharge volume, ions and electrons are rapidly lost by recombination, but the fast-flowing effluent still contains neutral metastable species (e.g., O2*, He*) and radicals (e.g., O, OH). This reactive effluent has been shown to be an effective neutralizer of surrogates for anthrax spores and mustard blister agent. Unlike conventional wet decontamination methods, the plasma effluent does not cause corrosion and it does not destroy wiring, electronics, or most plastics, making it highly suitable for decontamination of sensitive equipment and interior spaces. Furthermore, the reactive species in the effluent rapidly degrade into harmless products leaving no lingering residue or harmful by-products.
Oligodendrocyte-Specific Protein Peptides Induce Experimental Autoimmune Encephalomyelitis in SJL/J Mice (1999)

Oligodendrocyte-specific protein (OSP) is a recently isolated and cloned, 207-aa, hydrophobic, four-transmembrane protein found in CNS myelin. It represents approximately 7% of total myelin protein. The OSP cDNA sequence has no significant homology with previously reported genes, but the predicted protein structure suggests that OSP is a CNS homologue of peripheral myelin protein-22. We previously reported the presence of anti-OSP Abs in the cerebrospinal fluid of relapsing-remitting multiple sclerosis (MS) patients, but not control patient groups. In this study, we tested the ability of a panel of 20-mer peptides with 10-aa overlaps, representing the sequence of murine OSP, to induce experimental autoimmune encephalomyelitis (EAE), an animal model for MS. SJL mice challenged with murine OSP peptides 52-71, 82-101, 102-121, 142-161, 182-201, and 192-207 exhibited clinical EAE. OSP:52-71 elicited severe relapsing-remitting EAE in some individuals. All other encephalitogenic peptides elicited, at most, a loss of tail tonicity from which the mice most often completely recovered. Mononuclear cell infiltrates and focal demyelination characteristic of EAE were evident. T cell proliferative responses were seen with all encephalitogenic peptides except 142-161 and 182-201. OSP peptides 72-91 and 132-151 did not cause clinical EAE, but did elicit robust proliferative responses. B10.PL and PL/J mice challenged with the same OSP peptide doses as SJL mice did not exhibit clinical EAE. These results in the SJL EAE model, together with the results from MS patient clinical samples, make OSP a promising candidate for autoantigenic involvement in MS.
Listen, Attend and Spell (2015)

We present Listen, Attend and Spell (LAS), a neural network that learns to transcribe speech utterances to characters. Unlike traditional DNN-HMM models, this model learns all the components of a speech recognizer jointly. Our system has two components: a listener and a speller. The listener is a pyramidal recurrent network encoder that accepts filter bank spectra as inputs. The speller is an attention-based recurrent network decoder that emits characters as outputs. The network produces character sequences without making any independence assumptions between the characters. This is the key improvement of LAS over previous end-to-end CTC models. On a subset of the Google voice search task, LAS achieves a word error rate (WER) of 14.1% without a dictionary or a language model, and 10.3% with language model rescoring over the top 32 beams. By comparison, the state-of-the-art CLDNN-HMM model achieves a WER of 8.0%.
A Simple Short Synthesis of Isotachin ‘C’ (1990)

Abstract A short simple synthesis of Isotachin ‘C’ a sulphur containing aromatic ester isolated from New-Zealand Liver worts, Balantiopsis rosea has been described.
Flexible data authentication evaluated for the smart grid (2013)

This paper explores Time-Valid One-Time-Signature (TV-OTS) as a data authentication protocol for potential use in smart grid applications. TV-OTS is highly configurable with computationally lightweight signing and verification processes, making it a strong candidate for smart grid use. A detailed analysis of security against brute force attacks is presented, which is critical to understanding the parameters under which TV-OTS is reliably secure. This analysis is used to choose applicable parameters for latency tests of a full TV-OTS implementation. Performance results are favorable, with the cost of combined signing and verifying reaching under 10 milliseconds.
Quantitative structural activity relationship study of bis-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors (1995)

This work describes a study of quantitative structural activity relationships (QSAR) of bis-tetraazamacrocyclic compounds. These compounds represent a novel class of very potent and selective anti-HIV inhibitors, with a new mode of action. The QSAR study correlates structural features of the compounds with anti-HIV activity, resulting in a model which has a high predictive capacity (predictive r2 = 0.79). This predictive model will be of major importance for the design of new anti-HIV inhibitors of this class. Use is made of partial least-squares (PLS) analysis, with the novelty being that structural features derived by inclusion of all sterically allowed conformations for each molecule are included in the analysis. PLS analysis was made of descriptors, including structural parameters, macrocyclic ring size, metal chelating ability, etc., and those features necessary for the observed antiviral activities of these compounds were deduced from the models. Since all sterically allowed conformations are included in the analysis, the flexibility of the molecules is also taken into account. In addition, a correlation is found (indicated by a predictive r2 value of 0.61) between inhibition of HIV-1 (HIV-2) and syncytium formation inhibition in the presence of bis-cyclam analogues, leading to the suggestion of a common target, namely, gp120, being involved in both inhibition of virus replication and syncytium formation.
TMZ-BioShuttle – a reformulated Temozolomide (2008)

There is a large number of effective cytotoxic drugs whose side effect profile, efficacy, and long-term use in man are well understood and documented over decades of use in clinical routine e.g. in the treatment of recurrent glioblastoma multiforme (GBM) and the hormone-refractory prostate cancer (HRPC). Both cancers are insensitive against most chemotherapeutic interventions; they have low response rates and poor prognoses. Some cytotoxic agents can be significantly improved by using modern technology of drug delivery or formulation. We succeeded to enhance the pharmacologic potency with simultaneous reduction of unwanted adverse reactions of the highly efficient chemotherapeutic temozolomide (TMZ) as an example. The TMZ connection to transporter molecules (TMZ-BioShuttle) resulted in a much higher pharmacological effect in glioma cell lines while using reduced doses. This permits the conclusion that a suitable chemistry could realize the ligation of pharmacologically active, but sensitive and highly unstable pharmaceutical ingredients without functional deprivation. The re-formulation of TMZ to TMZ-BioShuttle achieved a nearly 10-fold potential of the established pharmaceutic TMZ far beyond the treatment of brain tumors cells and results in an attractive reformulated drug with enhanced therapeutic index.
Totalsynthese optisch aktiver Steroide, XI. Synthese von (—)‐Des‐A‐Steroiden (1975)

Optisch aktive (7aS)-7a-Alkyl-5,6,7,7a-tetrahydroindan-1,5-dione 1 werden durch Anbau einer Ketobutylseitenkette zu 4, Umwandlung in die Cyclopenta[f][1]benzopyrane 13, selektive Hydrierung und Hydrolyse-Ringschlußreaktion in (−)-Des-A-Steroide 17 übergeführt. Total Synthesis of Optically Active Steroids, XI. Synthesis of (—)-De-A-Steroids Optically active (7aS)-7a-alkyl-5,6,7,7a-tetrahydro-indan-1,5-diones 1 were transformed in to (−)-de-A-steroids 17 by introduction of a ketobutyl-side chain to give 4, conversion to the cyclopenta[f][1]benzopyranes 13, selective hydrogenation, and hydrolysis ring closure reaction.
Moricizine Bioavailability via Simultaneous, Dual, Stable Isotope Administration: Bioequivalence Implications (1999)

The relative bioavailability of a 200 mg film-coated tablet of [12C]moricizine.HCl in comparison to a 200 mg [13C6]moricizine.HCl oral solution was determined after simultaneous administration to 8 young healthy male subjects. Concentrations of [12C]moricizine.HCl and [13C6]moricizine.HCl were determined by thermospray liquid chromatography-mass spectrometry (LC-MS) using [2H11]moricizine.HCl as the internal standard. The mean absorption and disposition parameters of the tablet versus the solution were the following (%CV): maximum concentration, 0.83 (39%) versus 0.79 (39%) microgram/mL; time of maximum concentration, 0.81 (40%) versus 0.65 (28%) hours; area under the concentration-time curve (AUC), 1.58 (39%) versus 1.49 (37%) micrograms.h/mL; apparent oral clearance, 150.7 (52%) versus 158.1 (50%) L/h; and t1/2, 1.9 (42%) versus 1.9 (42%) hours. The AUC for the tablet averaged 106% of the solution, which likely reflects a greater first-pass effect with the oral solution. Partitioning sources of variation confirmed the low (< 6%) intrasubject coefficient of variation (cv epsilon) afforded via the single-period, dual-isotope design. In contrast, a previous study using the conventional two-period crossover design determined the cv epsilon about moricizine metrics to be in excess of 30%, resulting in classification of this drug as having highly variable absorption. The results of this study further illustrate the benefits of dual, stable isotopes to assess bioavailability and bioequivalence. This paradigm results in a reduction in experimental time and subject inconvenience and lower costs in comparison with the standard crossover study. Perhaps most important is the improved statistical power for the evaluation of bioavailability or bioequivalence in the absence of period and sequence effects that confound the assessment of intrasubject variation in the standard crossover design.
Fluorescence Assays for High-Throughput Screening of Protein Kinases (2003)

Protein kinases comprise one of the most important group of targets for drug discovery research today. Methods to identify novel kinase inhibitors by high-throughput screening have evolved rapidly in recent years. An important aspect is the availability of fluorescent probes that can be applied in a homogeneous, or mix-and-measure, assay format. Here, we illustrate the application of fluorescence read-out technologies for kinase targets in light of our own experiences in assay development and high-throughput screening. Keywords: fluorescence assays, high-throughput screening, protein kinases, novel kinase inhibitors
Genetic and phenotypic characterization of cop1 mutants of Arabidopsis thaliana (1992)

Summary Ten Arabidopsis lines that carry recessive mutations in the cop 1 (constitutively photomorphogenic) locus have been isolated. These lines define at least four different alleles. All of the mutant lines produce dark‐grown seedlings that mimic wild‐type seedlings grown in the light. The phenotype of the dark‐grown mutant seedlings includes: short hypocotyls, open and enlarged cotyledons, accumulation of anthocyanin, cell‐type differentiation and chloroplast‐like plastid differentiation in cotyledons. Moreover, in more prolonged dark‐growth periods the mutants exhibit true leaf development that parallels that in light‐grown siblings. The four mutant alleles represent two types of mutations: three alleles ( cop 1‐1, cop 1‐2, and cop 1‐3) have severely affected phenotypes whereas one allele ( cop 1‐4) has a less severe phenotype. Compared to the severe alleles, the cop 1‐4 mutant has slightly longer hypocotyls in dark‐grown seedlings and does not accumulate abnormal levels of anthocyanin. The cop 1–1/ cop 1‐4 hybrid seedlings are intermediate in many physiological properties under both dark‐ and light‐growth conditions, relative to the two parents. These results may suggest that the extent of residual cop 1 gene activity in the mutants dictates the degree to which the aberrant plant phenotype is expressed. Analysis of plants carrying both cop 1 and hy , a mutation that results in a deficiency of active phyto‐chrome, suggests that the cop 1 gene product acts downstream of phytochrome. The differentiation of chloroplasts in the roots of light‐grown cop 1 plants but not in wild‐type plants suggests that the wild‐type cop 1 gene product also normally plays a role in suppressing chloroplast development in the roots of light‐grown plants. To aid the eventual molecular cloning of the cop 1 locus, its chromosomal location has been mapped and a molecular marker that is located about 1 centimorgan away from the cop 1 locus obtained.
Effect of two years' supplementation with natural antioxidants on vitamin and trace element status biomarkers: preliminary data of the SU.VI.MAX study. (2001)

The "SUpplementation en VItamines et Minéraux AntioXidants" (SU.VI.MAX) study is a randomized double-blind, placebo controlled, primary-prevention trial designed to test the efficacy of a daily supplementation with antioxidant vitamins (vitamin C, 120 mg; vitamin E, 30 mg; and beta-carotene, 6 mg) and minerals (selenium, 100 microg; and zinc, 20 mg) at nutritional doses (one to three times the daily recommended dietary allowances), in reducing the frequency of cancers and cardiovascular diseases. The study involves 12,735 eligible subjects (women aged 35-60 years, men aged 45-60 years) included in 1994 in France. They will be followed up for 8 years. The targeted population is the general population. The aim of this specific analysis is to assess the effect of 2 years of supplementation on biochemical indicators of vitamin and trace element on a subsample of 1000 subjects. The mean (+/- standard deviation) concentrations of plasma beta-carotene, alpha-tocopherol, vitamin C, selenium and zinc among participants who were randomly assigned to receive a daily supplementation with beta-carotene, vitamin E, vitamin C, selenium and zinc for 2 years were significantly higher than those who were assigned to receive placebo. Specifically, the mean concentrations among men in the intervention group were 0.86 +/- 0.70 micromol/L for beta-carotene, 35.3 +/- 9.3 micromol/L for alpha-tocopherol, 11.5 +/- 4.7 microg/ mL for vitamin C, 1.65 +/- 0.33 micromol/L for selenium, and 16.2 +/- 3.9 micromol/L for zinc. The mean concentrations among women in the intervention were 1.25 +/- 0.90 micromol/L for beta-carotene, 34.9 +/- 8.4 micromol/L for alpha-tocopherol, 12.6 +/- 4.0 microg/mL for vitamin C, 1.68 +/- 0.37 micromol/L for selenium, and 15.3 +/- 3.9 micromol/L for zinc. The values observed for beta-carotene and vitamin E in the supplementation group after 2 years of intervention are those that have been associated with the lowest risk of cancer in observational studies. They are definitely lower than concentrations reported in intervention studies showing an apparent negative effect of high levels of beta-carotene supplementation on the lung cancer incidence rate in high-risk subjects (initial level multiplied by 12-18). Data from the follow-up will ascertain if any plausible reduction in the incidence rate of cancers may be associated with such amounts of antioxidant agents.
Expression and Prognostic Significance of Metalloproteinases and Their Tissue Inhibitors in Patients With Small-Cell Lung Cancer (1999)

MMPs and TIMPs are widely expressed in SCLC. Increased tumoral expression of MMP-3, -11, and -14 were independent negative prognostic factors for survival. The results support the evaluation of synthetic MMP inhibitors in patients with SCLC.
[In vitro study of the role of various preservation methods on mechanical properties of allografts of the patellar tendon]. (1991)

Tendon allografts are presently used for surgical reconstruction of the anterior cruciate ligament. The aim of this study was the in vitro evaluation of the modification of the mechanical properties of conserved human patellar tendons, deep-frozen or freeze-dried and sterilized with gamma rays. Thirty pairs of patellar tendons (central third) with their bony attachments were removed from fresh corpses, frozen in liquid nitrogen, then conserved at -80 degrees C. Out of each pair, one tendon was submitted to an additional treatment and the other was used as a control. Three types of treatment were studied: 2.5 Mrad irradiation (groupe I), freeze-drying with 1% residual humidity (groupe II), consecutive freeze-drying and irradiation (group III). After warming up (controls and group I treated tendons), the specimens were submitted to mechanical tests on the pulling machine with a suitable arrangement. Two types of tests were performed: a creep test (80 cycles at 1 Hz between 0 and 50 N) then an ultimate tensile strength test (0.25 mm/s). Freeze-drying causes macroscopic morphological alterations, which are even more marked if irradiation is applied in addition. The three types of treatment induce an increase in creep and a decrease in the ultimate, tensile strength and in Young's module, all being statistically significant. The three types of treatment alter the mechanical properties of the allograft. Freeze-drying maintains a better resistance of the graft. The combination of freeze-drying and irradiation is the most damaging method, and freeze-drying even seems to potentialize the harmful effects of irradiation resistance (group II freeze-dried grafts), the treated allografts present with changes in their viscoelastic properties that are incompatible with their clinical use. This study has also shown that some parameters influence the extent of the damaging effects of these three treatments, and experiments are being continued to optimize the conservation and sterilization procedure.
Electric characteristics of a surface barrier discharge with a plasma induction electrode (2006)

Static and dynamic current-voltage and charge-voltage characteristics of a surface barrier discharge with a plasma induction electrode have been investigated experimentally. The dependences of the discharge current on both the gas pressure in the induction electrode tube and the winding pitch of the corona electrode, as well as of the discharge power efficiency on the applied voltage, have been measured.
<title>Distortion-invariant optical pattern recognition using composite binary filters</title> (1993)

A method for constructing limited, distortion-invariant, composite, binary filters for an optical nonlinear joint transform correlator is described. Experimental results are presented on the in- situ construction of such filters, their invariance, discrimination, and correlation quality.
Determination of the efficacy of terbinafine hydrochloride nail solution in the topical treatment of dermatophytosis in a guinea pig model (2008)

Currently available topical antifungals are often not satisfactory for the treatment of nail infections, because of the inability to penetrate the nail plate. Terbinafine HCl nail solution is a novel antifungal formulation containing a nail penetration enhancer dodecyl-2-N,N-dimethylaminopropionate hydrochloride (DDAIP HCl, trade name NexACT-88). In this study, we used a guinea pig model of Trichophyton mentagrophytes dermatophytosis and evaluated the clinical and mycological efficacy of different terbinafine HCl nail solutions (TNS) formulated with or without DDAIP HCl. Ciclopirox (8%) nail lacquer (Penlac), the only Food and Drug Administration approved topical treatment for onychomycosis, was used as a comparator. Following the IACUC Guidelines, the skin of male albino guinea pigs was abraded under anaesthesia. Each animal was infected with T. mentagrophytes ATCC 24953 (cell suspension containing 1 x 10(7) conidia). The experimental animals were divided into 11 groups (five animals per group) and tested with the following formulations: vehicle control, 0.5% DDAIP HCl, 1%, 5% and 10% TNS (without DDAIP HCl), 1% TNS with 0.5%, 2.5% and 5.0% DDAIP HCl, 5% and 10% TNS with 0.5% DDAIP HCl, 8% ciclopirox nail lacquer and an untreated control group. Evaluation of clinical and mycological efficacy was performed 72 h after completion of a 7-day treatment regimen. Skin biopsy samples were processed for histopathological examination. The infected untreated control guinea pigs showed patches of hair loss and ulcerated or scaly skin and fungal invasion of hair roots. The vehicle and 0.5% DDAIP HCl treated groups showed minimal clinical efficacy (only 11% and 5%, respectively). In contrast, all three concentrations of TNS (1%, 5% and 10% terbinafine HCl) formulated with or without 0.5% DDAIP HCl showed 100% mycological efficacy by the hair root invasion test. Clinical efficacy of the 5% and 10% TNS improved with addition of 0.5% DDAIP HCl (47.4% and 73.8% vs. 68.4% and 89.5%, respectively). In addition, no fungal elements were detected in the treated guinea pig skin. All formulations of TNS resulted in a higher clinical and mycological efficacy compared with the 8% ciclopirox nail lacquer (P = 0.0444). In conclusion, TNS containing 1%, 5% and 10% terbinafine HCl formulated with and without DDAIP HCl demonstrated high antifungal efficacy in experimental dermatophytosis. Addition of 0.5% DDAIP HCl to 5% and 10% TNS significantly enhanced the clinical and mycological efficacy of these formulations which were superior compared with the 8% ciclopirox nail lacquer. Evaluation of the 1%, 5% and 10% TNS in clinical trials for the treatment of dermatophytosis and onychomycosis is warranted.