1,030 research outputs found

    Towards an Abstract Domain for Resource Analysis of Logic Programs Using Sized Types

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    We present a novel general resource analysis for logic programs based on sized types.Sized types are representations that incorporate structural (shape) information and allow expressing both lower and upper bounds on the size of a set of terms and their subterms at any position and depth. They also allow relating the sizes of terms and subterms occurring at different argument positions in logic predicates. Using these sized types, the resource analysis can infer both lower and upper bounds on the resources used by all the procedures in a program as functions on input term (and subterm) sizes, overcoming limitations of existing analyses and enhancing their precision. Our new resource analysis has been developed within the abstract interpretation framework, as an extension of the sized types abstract domain, and has been integrated into the Ciao preprocessor, CiaoPP. The abstract domain operations are integrated with the setting up and solving of recurrence equations for both, inferring size and resource usage functions. We show that the analysis is an improvement over the previous resource analysis present in CiaoPP and compares well in power to state of the art systems.Comment: Part of WLPE 2013 proceedings (arXiv:1308.2055

    Synthesis and study of biological activity of tetrahydro-1H-[3]-benzazepines

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    The 3-Benzazepines are an important class of compounds in drug discovery due to their biological activity such as analgesic, antihypertensive or anticancer properties as well as dopaminergic or antidopaminergic activity. In particular, the tetrahydro-1H-[3]- benzazepine is a common skeleton in a number of natural and pharmaceutical products. As consequence of the interesting biological properties, derivatives of the tetrahydro-1H-[3]-benzazepines, especially the 1-aryl substituted have been synthesized by different routes and evaluated their pharmacologic activity. [1,2] The stereoselective synthetic approaches of tetrahydro-1H-[3]-benzazepine have focused on ring enlargements, as the Stevens rearrangement (SR) which is a good regio- and diastereoselective synthetic methodology. In my research group, the reaction conditions to synthesize tetrahydro-1H-[3]-benzazepines 1,2-disubstituted by via SR from tetrahydroisoquinolinium salts conveniently functionalized have been optimized. [3,4] This methodology allowed us to obtain a wide variety of tetrahydro-1H-[3]- benzazepines 1,2-disubstituted with different substituents at A-ring (Cl, OMe) and the C-1 (-C6H4X, X = H, OMe, Cl, NO2, NMe2, NH2, SMe) and C-2 (Electron-withdrawing groups) positions. The demethylation of the synthesized tetrahydroisoquinolines and tetrahydro-1H-[3]-benzazepines 1,2-disubstituted, lead us to get catechol structure, an important requirement for their dopaminergic activity. We have studied the dopaminergic activity of the synthesized compounds by radioligand binding assays, establishing a structure-activity relationships. Literature: [1] A. Gini, Adv. Synth. Catal. 2016, 358, 4049. [2] H. Damsen, Eur. J. Org. Chem. 2015, 36, 7880. [3] M. Valpuesta, Eur. J. Org. Chem. 2010, 23, 4393. [4] M. Ariza, Eur. J. Org. Chem. 2011, 32, 6507.Universidad de Málaga. Campus de Excelencia Internacional Andalucía Tech

    Synthesis of bioactive compounds. Studies of their attachment to nanoparticles

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    The 1-aryl tetrahydroisoquinolines have attracted great attention in medicinal chemistry due to their biological activity. These compounds present antitumor, anti-HIV and antibacterial activities. Several analogues of 1-aryl tetrahydroisoquinoline are used for the treatment of neurodegenerative diseases such as Parkinson´s and Alzheimer´s diseases since also act as dopaminergic antagonists and N-methyl-D-aspartate receptor antagonist. [1] The 1-substituted tetrahydro-3-benzazepines have also been studied for their affinity to the Phencylclidine binding site of the NMDA receptor as well as for their affinity to the dopaminergic receptors. [2] In the last years, various methods have been carried out to satisfy the demand of novel tetrahydroisoquinolines and tetrahydro-3-benzazepines. We have synthesized nor-1-aryl tetrahydroisoquinolines with different substituents in the aryl group of C-1 (H, NMe2, SMe, NO2, NH2). In addition to this, we have performed the synthesis of nor-tetrahydro-3-benzazepinas by different routes, obtaining the best results via opening of epoxides by arylphenethylamines and subsequent cyclization. The nor-tetrahydroisoquinolines and nor-tetrahydro-3-benzazepines have been derivatized to obtain appropiate adsorbates which can be attached to nanoparticles. This fact is crutial in drug delivery systems as well as in the improvement of the biocompatibility of these compounds. Literature: [1] Toshiaki Saitoh, Eur. J. Med. Chem. 2006, 41, 241. Mattias Ludwig, Eur. J. Med. 2006, 41, 1003. [2] Olaf Krull, Bioorg. Med. Chem. 2004, 12, 1439.Universidad de Málaga. Campus de Excelencia Internacional Andalucía Tec

    Educational innovation on collaborative learning with CmapTools in the initial teacher training

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    Entre las principales destrezas que debería desarrollar actualmente el profesorado durante el proceso de formación inicial, podemos destacar el uso educativo de las Tecnologías de la Información y la Comunicación (TIC), el trabajo en equipo y la capacidad para reflexionar sobre el propio conocimiento. Para colaborar al desarrollo de tales aspectos hemos llevado a cabo un proyecto de innovación docente donde los estudiantes de magisterio aprenden a realizar mapas conceptuales individuales y grupales, con ayuda de CmapTools. Este software es libre y útil para integrar de forma práctica las TIC en el proceso educativo, ya que permite desarrollar una metodología activa, en la que se fomenta al mismo tiempo el aprendizaje reflexivo y el trabajo en equipo. Tras analizar los datos recogidos hemos observado que los futuros maestros muestran opiniones positivas sobre las estrategias y recursos empleados en esta experiencia, valorando especialmente el proceso de aprendizaje colaborativo desarrollado en el aula

    Comparative study of dopaminergic activity of tetrahydro-1H-[3]-benzazepines and their precursors

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    The discovery of the tetrahydro-1H-[3]-benzazepine SCH23390 [1], represented one of the most important advances in the study of dopaminergic receptors due to their behavior as a selective D1 receptor antagonist. The high affinity and selectivity of this tetrahydro-1H-[3]-benzazepine has led to the search for new structures because of their potential dopaminergic activity, especially 1-aryl-substituted tetrahydro-1H-[3]-benzazepines. Furthermore, their precursors, the tetrahydroisoquinolines 1-substituted have shown to have activity for D1 and D2 dopaminergic receptors.[2] We have carried out the synthesis of tetrahydro-1H-[3]-benzazepines 1,2-di-substituted by Stevens rearrangement (SR) on tetrahydroisoquinolinium salts. Stevens rearrangement is an efficient regio- and diastereoselective synthetic methodology. [3a,b] As part of our studies, we have performed the synthesis of benzazepines with modifications at the C-1 and C-2 positions with chlorine and hydroxyl groups at A-ring which is an important factor to modulate affinity at dopaminergic receptors. The interaction of these molecules with D1 and D2 dopaminergic receptors have been studied to establish a structure-activity relationship by radioligand binding assays.Universidad de Málaga. Campus de Excelencia Internacional Andalucía Tech

    Study and characterization of modified silicon surfaces with organic molecules

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    Nanostructured thin films and subsequent biofunctionalization of silicon substrates are essential for the development of biosensors devices. The formation of organic monolayers on silicon substrates via Si-C bound allows specific interactions with biomolecules and presents several advantages like greater detection sensitivity and stability against hydrolytic cleavage.1 In this sense, to control the orientation and spacing between grafted functional moieties on the surface, tripodal oligo (p-phenylene)s have become ideal anisotropic adsorbates due to their shape-persistent and selfstanding characteristics.2 On the other hand, biomolecules such as tehtahydro[3]benzazepines are well-known to contain in their structure a phenetylamine skeleton, which is also present in dopaminergic receptors and drugs, therefore these molecules have a remarkable interest in medicinal chemistry. Here we report the synthesis and characterization of several tetrahydro[3]benzazepines and tripod-shaped oligo(p-phenylene)s which were suitably functionalized for its subsequent adsorption on silicon surfaces by hydrosilylation and/or CuAAc click reaction. X-ray photoemission spectroscopy (XPS) and atomic force microscopy (AFM) analysis were also carried out to reveal the presence of the grafted molecules on the different Si surfaces.Universidad de Málaga. Campus de Excelencia Internacional Andalucía Tech

    Simplified calculations of slenderness limit in U.L.S. Of instability: interaction diagrams according to the instruction EHE-08

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    La introducción de la norma EHE-08 ha llevado consigo varios cambios, tanto conceptuales como paramétricos, en diferentes aspectos de su articulado. Este artículo busca ofrecer una ayuda al proyectista de hormigón, facilitándole los cálculos previos a la comprobación del Estado Límite de Inestabilidad. Se realiza una introducción al significado del límite inferior de esbeltez (incluyendo las propuestas de la ACI-318, el EC-2 y MC-90), para inmediatamente ofrecer una herramienta de aplicación directa que permita su obtención en el caso de la vigente Instrucción de hormigón estructural. Por otra parte, se expone también la formulación para comprobar secciones de soportes armadosRecent EHE-08 code has introduced many changes, both conceptual and parametric, in different aspects of its requirements. This paper seeks to offer support to the concrete designer, enabling pre-test calculations of the instability limit state. Beginning with an introduction to the meaning of the lower limit of slenderness (including ACI-318, EC-2 and MC-90 proposals), to immediately provide an application tool that allows obtaining direct in the case of the current Instruction of Structural Concrete. Moreover, it is also exposed the formulation to test reinforced column sections

    Mapping the potential distribution of frozen ground in Tucarroya (Monte Perdido Massif, the Pyrenees)

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    Producción CientíficaEste trabajo describe la metodología utilizada para cartografiar los suelos potencialmente helados en el valle de Tucarroya, en el Parque Nacional de Ordesa. Para cartografiar las formas asociadas a la presencia de hielo se combinó trabajo de campo, datos térmicos procedentes de sensores automáticos de temperatura del suelo y mediciones de la base del manto de nieve (BTS), así como variables predictivas obtenidas de un Modelo Digital de Elevaciones (MDE). La cartografía diferencia cuatro ambientes, suelo no congelado con actividad de la helada, suelos helados estacionales, permafrost posible y permafrost probable. El mapa revela una extensión del permafrost muy limitada, con escasez de formas asociadas. Solo se ha detectado por encima de los 2700 m de altitud en ambientes topográficos favorables, pendientessuaves y protegidos de la radiación solar. Los suelos helados estacionales son los ambientes más comunes y se desarrollan por encima de los 2500 m s.n.m., mientras los suelos no congelados,pero con heladas solo están presentes entre los 2570 y los 2750 m de altitud en laderas que reciben elevada radiación solarMinisterio de Economía, Industria y Competitividad - Fondo Europeo de Desarrollo Regional (projects CGL2015-68144-R / CGL2017-82216-R)Geoparque de Sobrarbe (project R- ADM15/57

    Recursos materials per al desenvolupament motor gros en escolars de 6-9 anys

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    L’objectiu de la recerca ha estat conèixer els recursos materials d’educació física més eficaços per millorar el desenvolupament motor gros de l’alumnat de 6 a 9 anys, en funció del seu sexe i edat. La mostra de 982 escolars es va dividir en tres grups experimentals segons el tipus de material fungible i un grup de control. Es va emprar el test TGM-2, mitjançant un pretest i un postest després d’una intervenció de 14 sessions. La diferència de puntuacions directes en els dos àmbits (locomotriu i control d’objectes) va ser major en els grups experimentals (p-valor<0,05). Aquesta diferència resulta més elevada amb l’ús de materials alternatius, seguit de només pilotes i sense pilotes en tots dos cicles educatius i en els dos sexes, excepte per a les nenes de segon cicle, on els millors resultats es produeixen en el grup experimental de materials només pilotes

    Recursos materiales para el desarrollo motor grueso en escolares de 6-9 años

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    El objetivo de la investigación ha sido conocer los recursos materiales de educación física más eficaces para mejorar el desarrollo motor grueso del alumnado de 6 a 9 años, en función de su sexo y edad. La muestra de 982 escolares estuvo dividida en tres grupos experimentales según el tipo de material fungible y un grupo de control. Se empleó el test TGM-2, mediante un pretest y un postest tras una intervención de 14 sesiones. La diferencia de puntuaciones directas en los dos ámbitos (locomotor y control de objetos) fue mayor en los grupos experimentales (p-valor<0,05). Dicha diferencia resulta más elevada con el uso de materiales alternativos, seguido de “solo balones” y “no balones” en ambos ciclos educativos y en los dos sexos, excepto para las niñas de segundo ciclo, donde los mejores resultados se producen en el grupo experimental de materiales “solo balones”
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