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

El reformismo despotista en la Universidad de Quito

Se analiza en este trabajo el limitado alcance que las reformas borbónicas tuvieron en las universidades hispanoamericanas, pese a algunos intentos. Se toma como ejemplo el caso de la Real Universidad de Santo Tomás de Quito y los proyectos de reforma presentados por el Barón de Carondelet, Presidente de la Real Audiencia de Quito, hacia 1800.This work examines the limited extend that the Borbonic reforms had on Hispanoamerican universities. The article examines the reforms presented by the Barón de Carondelet, president of the Real Audiencia de Quito in about 1800 for the Real Universidad de Santo Tomás de Quito.Publicad

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

Una universidad mayor que nunca tuvo estatutos : Santo Tomás de Quito. Funcionó con unas constituciones provisionales sin aprobación real y afrontó tres reformas estatutarias que jamás entraron en vigor

Ponencia en las IV Jornadas sobre la presencia universitaria española en América. Alcalá de Henares, Abril de 1990

Clásicos en vida. Las publicaciones de Jorge Juan y el reformismo borbónico en América

Peer reviewe

El espejo roto. Una polémica sobre la obra de Alejandro de Humboldt en la Venezuela del siglo XIX

Uno de los problemas más graves a los que tuvieron que hacer frente los Estados nacionales americanos, en lento trance de edificación durante el siglo XIX, fue el de la carencia de instituciones científicas. Estas fueron apoyadas, desde el punto de vista ideológico, con la creación de una nueva mitología científica. En el caso de Venezuela, el culto bolivariano se correspondió en lo científico con la devoción incontestable por la vida y la obra del sabio alemán Alejandro de Humboldt. Este panorama de aceptación general se rompió en 1867, cuando un viajero y político, Francisco Michelena, realizó una fuerte reprobación a la obra humboldtiana por sus "contradicciones" respecto a la frontera venezolana con Brasil. Contestado a su vez por el positivista Adolfo Ernst, la polémica entre ambos personajes nos muestra la estrecha relación entre la construcción nacional y la búsqueda y creación de mitos políticos y científicos en la América del siglo XIX

Discovering Rehabilitation trends in Spain: A bibliometric analysis

The main purpose of this study is to offer an overview of the rehabilitation research area in Spain from 1970 to 2018 through a bibliometric analysis. Analysis of performance and a co-word science mapping analysis were conducted to highlight the topics covered. The software tool SciMAT was used to analyse the themes concerning their performance and impact measures. A total of 3,564 documents from the Web of Science were retrieved. Univ Deusto, Univ Rey Juan Carlos and Basque Foundation for Science are the institutions with highest relative priority. The most important research themes are IntellectualDisability, Neck-Pain and Pain