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

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

Study and characterization of modified silicon surfaces with organic molecules

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

Rendimiento académico y calidad de vida relacionada con la salud en estudiantes de odontología

Objetivo: Asociar rendimiento académico y la calidad de vida relacionada con la salud (CVRS) en estudiantes de odontología, Universidad de Cartagena. Materiales y métodos: Estudio de corte transversal realizado en 347 estudiantes, previo consentimiento informado. Se diseñó y aplicó encuesta auto diligenciada para indagar variables sociodemográficas y CVRS ( WHOQOL-BREF). El rendimiento académico  fue obtenido a través de la secretaría académica de la institución. Se estimaron ocurrencias (prevalencias) y asociaciones entre variables (odds ratios) con un nivel de confianza del 95 % Resultados: 35,2 % de los estudiantes presentaron bajo rendimiento académico y los principales motivos de pérdidas de asignaturas fueron poco tiempo dedicado a estudiar (20,1%) y metodología académica utilizada (13,8%). Según el cuestionario WHOQOL-BREF, 37,7%   de los estudiantes percibió presentar una buena CVRS y sentirse bastante bien con su salud (52,2 %). Se encontró asociación entre los estudiantes con bajo rendimiento académico y compromiso del dominio social evaluado por el WHOQOL-BREEF (OR =2,13, IC 95 %=1,12-4,06 p=0,02) y ser adolescente (OR =1,7, IC 95 %=1,04-3,05 p=0,03). Conclusión: Se halló asociación entre bajo rendimiento académico y compromiso con el dominio social de los estudiantes en relación a CVRS y ser adolescente. El contexto universitario debe mirar de una manera holística el desarrollo académico del estudiante en aras del mejoramiento de su calidad de vida

El nuevo SIGPAC DEHESA, una herramienta fundamental en la aplicación de la nueva normativa de cerdo ibérico

El SIGPAC es un sistema de información geográfica que permite identificar las parcelas agrícolas de todo el territorio nacional, ahora con la nueva norma de calidad del cerdo ibérico añade una nueva capa, Montanera, que identifica las dehesas productoras de bellota. Se realiza el aforo de montaneras de cada parcela mediante la aplicación del modelo Dehesa previamente se determinan con un analizador de imágenes el número de encinas y la superficie que éstas ocupan

Effect of adding photoprotective compounds in the diet of Palaemon macrodactylus and its role under ultraviolet radiation

During the past two decades, it has shown an increase in ultraviolet radiation (UVR) and particularly the UVB (280-315nm) above Earth's surface. There is some evidence that UV-B radiation (280-315 nm) and the shorter wavelengths of UV-A (315-400 nm) can significantly affect the biota in waters up to 20 m deep and have adverse on aquatic organisms such as damage in the genetic material and high mortality. It has been shown that many species of seaweeds synthesize and accumulate high concentrations of photoprotective compounds and may constitute an interesting alternative as a supplement in aquaculture feeds. In the present work the effects of UVR were studied in the animal model Palaemon macrodactylus which is a successful invader, known as the Oriental Shrimp, native to estuaries and coastal waters of the Northwest Pacific. In the south western Atlantic, the species was found in Mar del Plata harbour, Argentina, probably introduced from the Pacific with discharged ballast water The aim of this study was to determine the bioaccumulation of photoprotective compounds (PPC) from diets added with red seaweeds meal of the family Halymeneaceae on juvenile P. macrodactylus and its possible protective role under conditions of stress by UVR. Juveniles of P. macrodactylus collected from Mar del Plata harbour (38° 03′ S; 57° 31′ W) were placed in PVC tanks under controlled conditions of temperature, pH, and salinity, under two feeding treatments: one group with basal diet (B) (45% protein, 8% lipid, 7% water and 7% ash) and the other 2% diet added with red seaweed meal of the family Halymeneaceae (diet B2). After 15 days animals were subjected to two radiations in four treatments, by triplicate: a) Control PAR (400-700nm) and diet B b) PAR+ UVR (280-700nm) and diet B c) PAR and diet B2, d) PAR+ UVR and diet B2. Survival, percentage of weight gain, concentrations of PPC and carotenoids were determined. In treatment b mortality of 16% was recorded after 72 hours of exposition to UVR, while in those fed with the 2% added diet, the same mortality was observed after 120 h of exposure. Survival in the treatments (a, c) was 100%. At the end of the exposure radiation period, percentage of weight gain was higher in animals fed with diet B (77%) nevertheless concentration of PPC and carotenoids (determined as OD g tissue-1) recorded the highest values in the animals corresponding to treatment c (PPC: 1.9 ± 0.38 DO g-1; carotenoids: 0.48 ± 0.1 OD g-1). although there were no significant differences between other treatments. These results suggest that, a diet added with red seaweeds rich in photoprotective compounds constitutes and interesting alternative, not only for its contribution to a better physiological state of animals under stress conditions by UVR, but also for the particularity of being invasive species with potential commercial use

Comparación del índice de vegetación de diferencia normalizada obtenido a diferentes escalas en pastos de dehesa

Las imágenes satelitales son una importante fuente de información para el seguimiento de la vegetación y de la cartografía de la tierra en varias escalas. Varios índices de vegetación se han empleado para evaluar la calidad y cantidad de la vegetación utilizando datos satelitales. Dado que las características de las bandas espectrales del infrarrojo cercano (NIR, radiación reflejada en la longitud de onda 800 nm) y el rojo (RED, radiación reflejada en la longitud de onda 670 nm) son muy distintas según el tipo de sensor, los valores del Índice de Vegetación de la Diferencia Normalizada (NDVI) variarán según el tamaño del píxel y de la heterogeneidad y la escala de las superficies. Se seleccionaron dos zonas de dehesa (Salamanca y Córdoba) y se tomaron imágenes mensuales del satélite DEIMOS-1 con una resolución espacial de 22 m × 22 m. El objetivo de este estudio es establecer una comparación entre diferentes resoluciones, mediante los valores de NDVI obtenidos en diferentes épocas del año en el que la actividad fotosintética de las plantas varía. Los resultados a diferentes escalas mostraron un comportamiento fractal del NDVI por lo que puede concluirse que las áreas de pasto herbáceo evaluadas presentan un comportamiento homogéneo

Avaliação de reativos padrões para provas de Imunodifusão Radial. Controle in vitro de vacinas antirrábicas

The RID assay is one of the in vitro methods used for in-process control in the production of rabies vaccines for veterinary use. It has been shown to be very useful for determining antigen concentration in the final bulk product. The work presented in this paper, including the production and standardization of candidate standard reagents for use in the Radial Immunodiffusion Assay (RID) was carried out at the Pan American Institute for Food Protection and Zoonoses (INPPAZ/PAHO/WHO). The study was completed with the cooperation of the Faculty of Veterinary Sciences, National University of La Plata (NULP), Argentina, where the validation of the proposed standards and the quality control of samples from 28 different batches of rabies vaccines produced with Pasteur strain rabies virus (PV) in BHK cells were performed. The activity of the vaccines was determined by in vivo (NIH) and in vitro (RID)assays. The results of the candidate reagents for the reagent standardization tests showed stability, sensitivity and reproducibility. The Relative Potency the 1.2 between the problem vaccines and the reference vaccine was estimated by variance and regression analysis. The results of our validation study show that the INPPAZ (PAHO/WHO) is capable of producing and distributing the above-mentioned standard reagents, as well as of providing support for the incorporation of the RID technique (sensitive, rapid and inexpensive) to the laboratories that manufacture rabies vaccines in Latin America and the Caribbean.A prova de Imunodifusão Radial (IDR) é um método in vitro conveniente para determinar a concentração de antígenos no produto final como um todo, de vacinas anti-rábicas para uso veterinário. Os reativos padrões candidatos para uso na prova IDR, proposta para o controle de processo de vacinas de cultivo celular, elaboradas na América Latina e Caribe, foram produzidos e padronizados no Instituto Panamericano de Proteção de Alimentos e Zoonoses (INPPAZ). A validação dos padrões e o controle de qualidade de 28 lotes de vacinas anti-rábicas, de diferentes procedências, foram realizados na Faculdade de Ciências Veterinárias da Universidade de La Plata, Argentina (UNLP). Todas as vacinas foram elaboradas com virus rábico cepa Pasteur (PV) em células BHK e sua atividade foi determinada através de provas in vivo (NIH) e in vitro (IDR). Os resultados dos reativos, candidatos para as provas de padronização, demonstraram estabilidade, sensibilidade e reprodutibilidade. Por análise de variância e de regressão foi estimada a potência relativa de 1.2 entre as vacinas problemas e a vacina de referência. Os resultados deste estudo de validação indicam que o INPPAZ, está em condições de elaborar e distribuir os reativos padrões acima mencionados e apoiar a adoção da técnica de IDR (sensível, rápida, econômica) pelos laboratórios de produção de vacinas anti-rábicas da América Latina e Caribe

Determinantes para la selección de la alternativa de financiación de vivienda no Vis en Colombia

Investigación que busca determinar las principales características y variables sociodemográficas que diferencian a las personas que escogen el leasing sobre el crédito hipotecario para adquirir vivienda No Vis en Colombia.Planteamiento del Problema, Pregunta de Investigación, Hipótesis, Objetivo General, Objetivos Específicos, Estado del Arte, Marco teórico, Metodología, Análisis descriptivo de los clientes que tomaron crédito de vivienda, Resultados Regresión Lineal, Resultados Regresión Logit.Magíster en Administración de Empresas, CESA.Maestrí