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

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

Kinetic Study of the Electrochemical Mineralization of m-Cresol on a Boron-Doped Diamond Anode.

The kinetics of the electrooxidation of m-cresol in aqueous solution was investigated in a one-compartment flow electrochemical cell with a boron-doped diamond electrode (BDD). Cyclic voltammograms recorded on BDD revealed that cresol oxidation takes place at a potential very close to the discharge of water. Under potentiostatic conditions, at a working potential lower than water discharge, a passive layer was rapidly formed on the electrode surface due to cresol polymerization. The anode fouling was not observed during electrolysis performed with the flow electrochemical cell operating under galvanostatic conditions. In this case, the decay of mcresol concentration followed a pseudo-first-order kinetics. The abatement of chemical oxygen demand (COD) showed that the kinetics of m-cresol oxidation was limited by mass transfer and that a full mineralization was achieved. A good agreement between predicted and experimental COD and instantaneous current efficiency values was obtained, although some deviations were observed at high current since the experimental data decreased faster than those predicted ones. These deviations can be explained by the occurrence of oxygen evolution which increases the mass transfer coefficient

Acción tutorial y clima escolar en los centros educativos a juicio del profesorado de Educación Secundaria Obligatoria

En este artículo se analiza cómo percibe el\ud profesorado la incidencia de la Acción Tutorial\ud en el Clima de Trabajo en los centros\ud educativos. Esta investigación viene\ud determinada por factores tan importantes\ud como comunicación, motivación y participación;\ud y otros de menor relevancia pero que no se\ud deben olvidar como la dirección del centro,\ud contexto, organización, planificación interna,\ud convivencia….Responde a la preocupación\ud por la mejora del sistema educativo español y\ud del funcionamiento de la organización\ud educativa, desde el estudio y conocimiento\ud riguroso.In this article it is analized the way that the\ud teaching staff perceives the tutorial staff\ud incidence in the working environment of the\ud centres.\ud This investigation is determined by important\ud factors as communication, motivation and\ud participation. There are also less important\ud factors, but they can’t be forgotten, for example\ud the direction of the center, context, organisation,\ud internal planning, coexistence…this is related\ud to the preoccupation about the improvement of\ud the Spanish educative system and the\ud development of the educative organisation\ud from the study and the rigorous knowledge

Optimization of urban mobility measures to achieve win-win strategies

European cities are essential in the development of Europe as they constitute the living environment of more than 60% of the population in the European Union and are drivers of the European economy – just under 85% of the EU’s gross domestic product is produced in urban areas (EC, 2007a). The car has been one of the main factors of development during the 20th century, but it is at the same time the origin of the key problems cities have to face: traffic increase. This has resulted in chronic congestion with many adverse consequences such as air pollution and noise. This loss of environmental quality is one of the reasons for urban sprawl in European cities during recent decades. But this urban sprawl at the same time worsens the environmental conditions. We must return to the dense city, but clean and competitive, and this implies reducing car use yet provides quality transport alternatives sufficient to recover and maintain the competitiveness of cities (EC, 2007a). Consequently, European cities need to establish an urban transport strategy which helps reduce their environmental problems –mainly emissions and noise – but without decreasing their trip attraction. This aspect is very important because a loss of trip attraction would result in an increase of people moving to more disperse areas, contributing towards worsening the current situation. This thesis is an attempt to contribute solutions to this problem in two ways: 1) The first is to analyze the complementarity and possible synergies of several urban transport measures aimed at improving a modal split to a more sustainable means of transport. This analysis will focus on the three aspects already mentioned: emissions, noise and attractiveness or competitiveness. 2) Once possible synergies and complementarities have been analyzed, the second objective is to propose the best combination of these measures, in terms of level of implementation, to achieve the maximum benefit with respect to the three aspects previously established: emissions, noise and attractiveness or competitiveness. Therefore, within the wide range of measures enhancing sustainable urban transport, three of them have been be selected in this thesis to establish a methodology for achieving these objectives. The analysis will be based on the region of Madrid, which is also the case study selected for this research. Las ciudades europeas son piezas fundamentales para el desarrollo europeo, ya que son el lugar de residencia de más del 60% de la población de la unión europea así como los motores de su economía – casi el 85% del PIB europeo se produce en áreas urbanas (EC, 2007a). El coche ha sido uno de los principales motores de desarrollo de las ciudades durante el siglo XX, pero se ha terminado por convertir a su vez en uno de los principales problemas con los que tiene que lidiar las ciudades: el aumento del tráfico. Esto ha derivado en unos niveles crónicos de congestión, con multitud de efectos adversos, entre los que cabe destacar la contaminación del aire y el ruido. Esta pérdida de calidad ambiental es una de las razones que ha propiciado la dispersión urbana que han experimentado las ciudades europeas en las últimas décadas. Pero esta dispersión urbana a su vez contribuye a empeorar las condiciones ambientales de las ciudades. Debemos retornar a la ciudad densa, pero limpia y competitiva, y esto implica reducir el uso del coche, pero proporcionando alternativas de transporte que permitan recuperar y mantener la competitividad de las ciudades (EC, 2007a). Por lo tanto, las ciudades europeas necesitan encontrar una estrategia de transporte urbano que ayude a reducir sus problemas medio ambientales – principalmente ruido y emisiones – pero sin hacerlas perder atractividad o competitividad. Este aspecto tiene gran importancia porque una pérdida de la misma se traduciría en un aumento de dispersión de la población hacia áreas periféricas, contribuyendo a empeorar la situación actual. Esta tesis contribuye a solucionar este problema de dos maneras: 1) La primera, analizando la complementariedad y posibles sinergias de diferentes medidas de transporte urbano orientadas a promover un reparto modal hacia modos más sostenibles. Este análisis se centrará en los tres aspectos anteriormente citados: emisiones, ruido y atractividad o competitividad. 2) Una vez las posibles sinergias y complementariedades se han analizado, el segundo objetivo es proponer la mejor combinación de estas medidas – en términos de grado de aplicación - para lograr el máximo beneficio en lo que respecta a los tres objetivos previamente establecidos. Para ello, en esta tesis se han seleccionado una serie de medidas que permitan establecer una metodología para alcanzar estos objetivos previamente definidos. El análisis se centra en la ciudad de Madrid y su área metropolitana, la cual se ha escogido como caso de estudio para realizar esta investigación

Synthesis of bioactive compounds. Studies of their attachment to nanoparticles

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

Lights and shadows of household satellite accouonts: the case of Catalonia, Spain

The construction of Household Satellite Accounts (HSAs) to value household production is not a new object of study. However, as their use has widened, research efforts have focused on resolving technical aspects of valuation assessment and far less attention has been paid to the underlying conceptual aspects. The purpose of this study is to contribute to improving the HSA as an analytical tool. Two approaches are proposed, drawing on existing data from Catalonia, Spain. The first approach involves incorporating the analysis of time as a key component of HSAs, making it possible to explore aspects of unpaid housework without the influence of monetary valuation. The second develops a new methodology that captures information on both housework and market work, overcoming some of the limitations of current databases used in the calculation of HSAs and allowing an analysis of the various interrelationships that exist between the two types of work

¿Un visionario del turismo o un gestor incompetente? El marqués de la Vega-Inclán, primer comisario regio de turismo

Es importante pararnos a pensar y plantearnos realmente cuáles son los orígenes de las políticas turísticas en nuestro país y si esas iniciativas realmente sentaron las bases de la política turística actual que tan buenos resultados está cosechando. Para ello vamos a viajar atrás en el tiempo hasta principios del siglo XX y dedicaremos este estudio a analizar la figura del II Marqués de la Vega Inclán, personaje clave en la historia turística española. A través de su biografía, del contexto cultural e histórico de la época, de su obra y de las opiniones que diferentes historiadores tienen de este personaje de principios de siglo descubriremos si era realmente un auténtico visionario o un gestor incompetente.Departamento de Historia Moderna, Contemporánea y de América, Periodismo y Comunicación Audiovisual y PublicidadGrado en Turism

Fair Coexistence of Scheduled and Random Access Wireless Networks: Unlicensed LTE/WiFi

We study the fair coexistence of scheduled and random access transmitters sharing the same frequency channel. Interest in coexistence is topical due to the need for emerging unlicensed LTE technologies to coexist fairly with WiFi. However, this interest is not confined to LTE/WiFi as coexistence is likely to become increasingly commonplace in IoT networks and beyond 5G. In this article we show that mixing scheduled and random access incurs and inherent throughput/delay cost, the cost of heterogeneity. We derive the joint proportional fair rate allocation, which casts useful light on current LTE/WiFi discussions. We present experimental results on inter-technology detection and consider the impact of imperfect carrier sensing.Comment: 14 pages, 8 figures, journa

Dissolved oxygen determination in two-dimensional tissue cultures using optical sensors

Oxygen concentration determination is of importance across many different industries, biomedical research among them. In biological systems, in vivo oxygen levels vary across a wide spectrum and strongly influence function of cells and tissues. Direct measurements of oxygen tension and its progression in real-time are necessary in order to understand and control cell survival, proliferation and differentation. In this thesis, special attention is payed to skin tissue. An in-depth understanding of these aspects will allow to provide better diagnostic and therapeutic tools for wound care. The general objective of this thesis is to analyze dissolved oxygen concentration in a two-dimensional tissue culture of a keratinocyte cell line (HaCaT) via the development and application to this purpose of an optical sensor. The sensor is based on a metalloporphyrin membrane (PtOEP) that emits a fluorescence signal that is quenched by oxygen in the environment. Images of the membrane are captured using time-lapse microscopy with a filter at the desired wavelength. Average pixel value is then analyzed, as it is directly related to O2 concentration. The porphyrin-based optical sensor developed in this work is proved to be compatible with cell culture. Using this sensor, changes in oxygen concentration in a physiological range can be detected. Dissolved O2 concentration in culture medium is found to decrease at high cell densities as a result of O2 consumption. It is also possible monitor discontinuities in a monolayer of cells by detection of local O2 concentration using this sensor.Ingeniería Biomédic

Population dynamics of Meloidogyne incognita on cucumber grafted onto the Cucurbita hybrid RS841 or ungrafted and yield losses under protected cultivation

The influence of the squash hybrid RS841 rootstock (Cucurbita maxima x C. moschata) on population dynamics of Meloidogyne incognita and yield of cucumber cv. Dasher II was assessed during 2013 and 2014 in a plastic greenhouse. In addition, the relationship between ecophysiological parameters (plant water status, gas exchange, and leaf reflectance) and Pi and cucumber yield were also estimated in 2013. Nematode densities were determined at the beginning (Pi) and at the end (Pf) of each crop, and the relationship between these parameters was used to estimate the maximum multiplication rate (a), the maximum population density (M) and the equilibrium density (E) per grafted and ungrafted cucumber and cropping season. Moreover, the relationship between the multiplication rate (Pf/Pi) and Pi was compared between grafted and ungrafted cucumber per cropping season. Finally, the relative yield of grafted or ungrafted cucumber was plotted against Pi to determine the tolerance limit (T) and the minimum relative yield (m) by the Seinhorst damage function model. Values of a, M and E in grafted cucumber were higher than in ungrafted one irrespective of the cropping season. These results were supported by comparing the relationship between Pf/Pi and Pi between grafted and ungrafted cucumber. The relationship between Pi and yield fitted the Seinhorst damage function. The values of T and m did not differ between grafted and ungrafted each year. Predawn water potential, net photosynthetic rate, and leaf chlorophyll index decreased with increasing Pi. In addition, relative yield was related to variation in net photosynthetic rate and the leaf chlorophyll index. Under the conditions of this study, RS841 rootstock was neither resistant nor tolerant to M. incognita.Postprint (published version