An Efficient Multi-component Synthesis of 6-Amino-3-methyl-4-Aryl-2,4- dihydropyrano[2,3-c]Pyrazole-5-carbonitriles

Multi-component reactions are effective in building complex molecules in a single step in a minimum amount of time and with facile isolation procedures; they have high economy1–7 and thus have become a powerful synthetic strategy in recent years.8–10 The multicomponent protocols are even more attractive when carried out in aqueous medium. Water offers several benefits, including control over exothermicity, and the isolation of products can be carried out by single phase separation technique. Pyranopyrazoles are a biologically important class of heterocyclic compounds and in particular dihydropyrano[2,3-c]pyrazoles play an essential role in promoting biological activity and represent an interesting template in medicinal chemistry. Heterocyclic compounds bearing the 4-H pyran unit have received much attention in recent years as they constitute important precursors for promising drugs.11–13 Pyrano[2,3-c]pyrazoles exhibit analgesic,14 anti-cancer,15 anti-microbial and anti-inflammatory16 activity. Furthermore dihydropyrano[2,3-c]pyrazoles show molluscidal activity17,18 and are used in a screening kit for Chk 1 kinase inhibitor activity.19,20 They also find applications as pharmaceutical ingredients and bio-degradable agrochemicals.21–29 Junek and Aigner30 first reported the synthesis of pyrano[2,3-c]pyrazole derivatives from 3-methyl-1-phenylpyrazolin-5-one and tetracyanoethylene in the presence of triethylamine. Subsequently, a number of synthetic approaches such as the use of triethylamine,31 piperazine,32 piperidine,33 N-methylmorpholine in ethanol,34 microwave irradiation,35,36 solvent-free conditions,37–39 cyclodextrins (CDs),40 different bases in water,41 γ -alumina,42 and l-proline43 have been reported for the synthesis of 6-amino-4-alkyl/aryl-3-methyl- 2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitriles. Recently, tetraethylammonium bromide (TEABr) has emerged as mild, water-tolerant, eco-friendly and inexpensive catalyst. To the best of our knowledge, quaternary ammonium salts, more specifically TEABr, have notbeen used as catalysts for the synthesis of pyrano[2,3-c]pyrazoles, and we decided to investigate the application of TEABr as a catalyst for the synthesis of a series of pyrazole-fused pyran derivatives via multi-component reactions

Improving Multi-class Text Classification with Naive Bayes

There are numerous text documents available in electronic form. More and more are becoming available every day. Such documents represent a massive amount of information that is easily accessible. Seeking value in this huge collection requires organization; much of the work of organizing documents can be automated through text classification. The accuracy and our understanding of such systems greatly influences their usefulness. In this paper, we seek 1) to advance the understanding of commonly used text classification techniques, and 2) through that understanding, improve the tools that are available for text classification. We begin by clarifying the assumptions made in the derivation of Naive Bayes, noting basic properties and proposing ways for its extension and improvement. Next, we investigate the quality of Naive Bayes parameter estimates and their impact on classification. Our analysis leads to a theorem which gives an explanation for the improvements that can be found in multiclass classification with Naive Bayes using Error-Correcting Output Codes. We use experimental evidence on two commonly-used data sets to exhibit an application of the theorem. Finally, we show fundamental flaws in a commonly-used feature selection algorithm and develop a statistics-based framework for text feature selection. Greater understanding of Naive Bayes and the properties of text allows us to make better use of it in text classification.

Lecture 2 - Java

Programming Overview The JVM (The Java Virtual Machine) A brief look at Structure Class Method Statement Magic incantations main() output Coding a Dog Programming Principle(1) If and Boolean operations Coding a Bank Account Quick look at ToolBox

TU Graz: Course: 707.000 Web Science and Web Technology: Lecture 13: Web Technologies 2 - The Semantic Web

The semantic web represents a current research effort to increase the capability of machines to make sense of content on the web. In this class, Peter Scheir will give a guest lecture on the basic principles underlying the semantic web vision, including RDF, OWL and other standards.

Class Test Generator

A combination of perl scripts and LaTeX files, this generates multiple multiple choice class tests from a single set of questions. You input a list of questions and answers into a text file. The script then produces any number of class tests that can be used, together with master answer sheets, by scrambling the order of the questions and the answers. Includes a detailed README file, but best just to try it and see.

Shared HLA Class II in Six Autoimmune Diseases in Latin America: A Meta-Analysis

The prevalence and genetic susceptibility of autoimmune diseases (ADs) may vary depending on latitudinal gradient and ethnicity. The aims of this study were to identify common human leukocyte antigen (HLA) class II alleles that contribute to susceptibility to six ADs in Latin Americans through a meta-analysis and to review additional clinical, immunological, and genetic characteristics of those ADs sharing HLA alleles. DRB1∗03:01 (OR: 4.04; 95%CI: 1.41–11.53) was found to be a risk factor for systemic lupus erythematosus (SLE), Sjogren’s syndrome (SS), and type 1 diabetes mellitus (T1D). DRB1 ¨ ∗04:05 (OR: 4.64; 95%CI: 2.14–10.05) influences autoimmune hepatitis (AIH), rheumatoid arthritis (RA), and T1D; DRB1∗04:01 (OR: 3.86; 95%CI: 2.32–6.42) is a susceptibility factor for RA and T1D. Opposite associations were found between multiple sclerosis (MS) and T1D. DQB1∗06:02 and DRB1∗15 alleles were risk factors for MS but protective factors for T1D. Likewise, DQB1∗06:03 allele was a risk factor for AIH but a protective one for T1D. Several common autoantibodies and clinical associations as well as additional shared genes have been reported in these ADs, which are reviewed herein. These results indicate that in Latin Americans ADs share major loci and immune characteristics.

Overcoming Gender Disadvantages. Social Policy Analysis of urban middle-class women in Colombia

The World Bank Report 2012 starts with this statement: “Gender equality matters in itself andit matters for development because, in today’s globalized worlds, countries that use the skillsand talents of their women would have an advantage over those which do not use it.” With theframe that suggest that gender equality matters, this paper describes some policy alternativesoriented to overcome gender disadvantages in the formal labor market incorporation of theurban middle class women in Colombia. On balance, the final recommendation suggest that itis desirable to adopt policy alternatives as Community Centers, which are programs orientedto a social redistribution of the domestic work as a way to encourage women participationin the formal labor market with the social support of the members of their own community.The problem that the social policy needs to address is the segregation of women in the formallabor market in Colombia. Although the evidence shows that the women overcome theeducational gap by showing better performance in education that their male peers, womenare still segregated of the labor market. The persistence of high rates of unemployment on thefemale population, the prevalence of the informal labor market as a women labor market, andthe presence of the payment difference between men and women with similar professionaltrainings are circumstances that sustain the segregation statement. These circumstances areinefficient for the society because an economic analysis shows that the cost of maintain the statuquo is externalized in the social security system that includes health, pension and maternityleave regimens. Therefore, the women segregation involves a market failure.This paper evaluates five policy alternatives each directed to the progress of a different causaldimension of the problem: (i) Quotas in the private market, (ii) Flexible working hours,(iii) replace the maternity leave with a family leave, (iv) Increase the Community Centers forredistributing the care work, and (v) Equal payment enforcement. The first alternative looksto increase women’s participation in the formal labor market. The second, third, and fourthalternatives constitute a package addressed at redistributing care work by reducing women’sresponsibility for reproductive work in the household with the help of husbands and the localgovernment. The fifth alternative intervenes to resolve the equal payment problem.After a four criteria evaluation that measure effectiveness, robustness and improbability inimplementation, efficiency and political acceptability or social opposition, the strongest alternativeis the fostering of Community Centers that promote a redistribution of care work. Thispolicy performs well in the assessment process because it combines gender focus with importantindirect effects: child support and human capabilities. The policy also shows a bottomup implementation process that overcomes the main adoption difficulties in the gender focusprograms and is supported by strong evidence of success in the Colombian context; this evidenceis produced by both transnational actors as a World Bank and also in local accountabilityreporters executed by local institutions like Colombian Institute of Family Welfare (ICBF).

Intersubject Units for the English Class. 'Unidades interdisciplinares para el aula de Inglés'.

Material para el alumnado de Educación Secundaria Obligatoria en el que se proponen cuatro unidades didácticas interdisciplinares en las que se trabaja un amplio abanico de temas transversales utilizando la lengua inglesa como vehículo de comunicación. La cuatro unidades propuestas son las siguientes: 1. The Same But Different, donde se trata el papel de la mujer en algunas civilizaciones contemporáneas, con un proyecto de trabajo final al que van dirigidas todas las actividades de la unidad; 2. Let's Talk About Sex, donde se tratan la pubertad, el sexo y la contracepción, informando al alumnado, que deberá hacer una elección libre y responsable entre las diferentes alternativas; 3. AIDS First Aid, donde se presenta una aproximación médica y social a la enfermedad; 4. Who Cares?, donde se trata el funcionamiento de un centro de salud británico y local, lo que supone que el alumnado deberá modificar y reelaborar sus esquemas de conocimiento, construyendo su propio aprendizaje. El diseño de las unidades didácticas incluye los objetivos, contenidos de las áreas curriculares implicadas así como los propios de la materia de Lengua Extranjera. Se incluyen multitud de actividades didácticas y unas hojas de autoevaluación diseñadas para que los alumnos tomen conciencia de su evolución, y en las que se evalúan los contenidos, el interés mostrado, el método de trabajo, la actitud hacia el tema, la dinámica de la clase y la labor del profesorado.

Society and class.

Forma parte de una serie que estudia la relación entre el arte y temas, situaciones, sentimientos e ideas que han alcanzado gran relevancia universal a lo largo de diferentes épocas y culturas y que se ha plasmado en manifestaciones como la fotografía, la pintura, la escultura, los textiles y el cine. Ayuda a saber interpretar las obras y estilos artísticos y entender el momento histórico en que fueron creados. Este volumen se centra en contar la vida de las personas, de las clases sociales y de sus relaciones, en todos los países y en todos los tiempos, desde los cazadores y agricultores prehistóricos representados en las pinturas rupestres hasta las obras de Andy Warhol en el siglo XX.

Biodegradation of the herbicide mecoprop-p with soil depth and its relationship with class III tfdA genes

Mecoprop-p [(R)-2-(4-chloro-2-methylphenoxy) propanoic acid) is widely used in agriculture and poses an environmental concern because of its susceptibility to leach from soil to water. We investigated the effect of soil depth on mecoprop-p biodegradation and its relationship with the number and diversity of tfdA related genes, which are the most widely known genes involved in degradation of the phenoxyalkanoic acid group of herbicides by bacteria. Mecoprop-p half-life (DT50) was approximately 12 days in soil sampled from <30 cm depth, and increased progressively with soil depth, reaching over 84 days at 70–80 cm. In sub-soil there was a lag period of between 23 and 34 days prior to a phase of rapid degradation. No lag phase occurred in top-soil samples prior to the onset of degradation. The maximum degradation rate was the same in top-soil and sub-soil samples. Although diverse tfdAα and tfdA genes were present prior to mecoprop-p degradation, real time PCR revealed that degradation was associated with proliferation of tfdA genes. The number of tfdA genes and the most probable number of mecoprop-p degrading organisms in soil prior to mecoprop-p addition were below the limit of quantification and detection respectively. Melting curves from the real time PCR analysis showed that prior to mecoprop-p degradation both class I and class III tfdA genes were present in top- and sub-soil samples. However at all soil depths only tfdA class III genes proliferated during degradation. Denaturing gradient gel electrophoresis confirmed that class III tfdA genes were associated with mecoprop-p degradation. Degradation was not associated with the induction of novel tfdA genes in top- or sub-soil samples, and there were no apparent differences in tfdA gene diversity with soil depth prior to or following degradation.

Inverse agonism of the antipsychotic drugs at the D-2 dopamine receptor

The antipsychotic drugs had been assumed to act as antagonists at D-2 dopamine receptors but recently these drugs have been shown to possess inverse agonist properties at this receptor. Inverse agonism may be demonstrated from the ability of these drugs to potentiate forskolin-stimulated cAMP accumulation or to suppress agonist-independent [S-35]GTPgammaS binding. The antipsychotic drugs tested generally appear as full inverse agonists in these assays regardless of chemical or therapeutic class. The mechanism of inverse agonism of the antipsychotic drugs is still unclear but may involve stabilisation of the ground state of the D-2 receptor. (C) 2003 Elsevier Science B.V All rights reserved.

Molybdenum eta(3)-allyl dicarbonyl complexes as a new class of precursors for highly reactive epoxidation catalysts with tert-butyl hydroperoxide

New Mo(II) diimine derivatives of [Mo(q (3)allyl)X(CO)(2)(CH3CN)(2)] (allyl = C3H5 and C5H5O; X = Cl, Br) were prepared, and [MO(eta(3)-C3H5)Cl(CO)(2)(BIAN)] (BIAN = 1,4-(4-chloro)phenyl-2,3-naphthalene-diazabutadiene) (7) was structurally characterized by single-crystal X-ray diffraction. This complex adopted an equatorial-axial arrangement of the bidentate ligand (axial isomer), in contrast with the precursors, found as the equatorial isomer in the solid and fluxional in solution. The new complexes of the type [Mo(eta(3)-allyl)X(CO)(2)(N-N)l (N-N is a bidentate chelating dinitrogen ligand) were tested for the catalytic epoxidation of cyclooctene using tert-butyl hydroperoxide as oxidant. All catalytic systems were 100% selective toward epoxide formation. While their turnover frequencies paralleled those of related Mo(eta) carbonyl compounds or Mo(VI) compounds bearing similar N-donor ligands, they exhibited similar olefin conversions in consecutive catalytic runs. The acetonitrile precursors were generally more active than the diimine complexes, and the chloro derivatives more active than the bromo ones. Combined vibrational and NMR spectroscopy and computational studies (DFT) were used to investigate the nature of the molybdenum species formed in the catalytic system with [Mo(eta(3)-C3H5)Cl(CO)(2){1,4-(2,6-dimethyl)phenyl-2.3-dimethyldiazabuta diene}] (4) and to propose that the resulting species may be dimeric bearing oxide bridges.