{"id":95102,"date":"2009-10-07T00:00:00","date_gmt":"2009-10-07T00:00:00","guid":{"rendered":"https:\/\/www.deberes.net\/tesis\/sin-categoria\/diseno-sintesis-evaluacion-de-la-actividad-biologica-y-farmacocinetica-de-nuevos-inhibidores-de-desacetilasas-de-histonas\/"},"modified":"2009-10-07T00:00:00","modified_gmt":"2009-10-07T00:00:00","slug":"diseno-sintesis-evaluacion-de-la-actividad-biologica-y-farmacocinetica-de-nuevos-inhibidores-de-desacetilasas-de-histonas","status":"publish","type":"post","link":"https:\/\/www.deberes.net\/tesis\/quimica-organica\/diseno-sintesis-evaluacion-de-la-actividad-biologica-y-farmacocinetica-de-nuevos-inhibidores-de-desacetilasas-de-histonas\/","title":{"rendered":"Dise\u00f1o, sintesis, evaluacion de la actividad biologica y farmacocinetica de nuevos inhibidores de desacetilasas de histonas"},"content":{"rendered":"<h2>Tesis doctoral de <strong> Dorleta Otaegui Ansa <\/strong><\/h2>\n<p>En la presente tesis se estudia el dise\u00f1o y la s\u00edntesis qu\u00edmica de una peque\u00f1a librer\u00eda de inhibidores de la familia de enzimas desacetilasas de histonas (hdac), as\u00ed como la evaluaci\u00f3n de la actividad biol\u00f3gica de dichos compuestos y estudios de farmacocin\u00e9tica de un compuesto seleccionado.  el dise\u00f1o del compuesto cabeza de serie se ha realizado mediante m\u00e9todos computacionales, tomando como base la estructura tridimensional de un an\u00e1logo de hdac de levadura.   la s\u00edntesis org\u00e1nica de los inhibidores se ha llevado a cabo mediante una ruta sint\u00e9tica en la que las etapas clave son las siguientes: reacciones de cicloadici\u00f3n [3+2] entre nitroalquenos e iluros de azometino metalados para obtener pirrolidinas altamente funcionalizadas, aromatizaci\u00f3n asistida por microondas para la obtenci\u00f3n de pirroles, reacciones de desprotecci\u00f3n y acoplamiento pept\u00eddico, y la obtenci\u00f3n del grupo \u00e1cido hidrox\u00e1mico quelante.  una vez sintetizada una familia de inhibidores con peque\u00f1as variaciones estructurales, se llev\u00f3 a cabo la evaluaci\u00f3n de la actividad biol\u00f3gica de las mol\u00e9culas sintetizadas, demostrando una potente capacidad inhibitoria por lo que se han llevado a cabo estudios de farmacocin\u00e9tica en ratones para determinar niveles del inhibidor tanto en plasma como en tejidos.<\/p>\n<p>&nbsp;<\/p>\n<h3>Datos acad\u00e9micos de la tesis doctoral \u00ab<strong>Dise\u00f1o, sintesis, evaluacion de la actividad biologica y farmacocinetica de nuevos inhibidores de desacetilasas de histonas<\/strong>\u00ab<\/h3>\n<ul>\n<li><strong>T\u00edtulo de la tesis:<\/strong>\u00a0 Dise\u00f1o, sintesis, evaluacion de la actividad biologica y farmacocinetica de nuevos inhibidores de desacetilasas de histonas <\/li>\n<li><strong>Autor:<\/strong>\u00a0 Dorleta Otaegui Ansa <\/li>\n<li><strong>Universidad:<\/strong>\u00a0 Pa\u00eds vasco\/euskal herriko unibertsitatea<\/li>\n<li><strong>Fecha de lectura de la tesis:<\/strong>\u00a0 10\/07\/2009<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n<h3>Direcci\u00f3n y tribunal<\/h3>\n<ul>\n<li><strong>Director de la tesis<\/strong>\n<ul>\n<li>Fernando Pedro Cossio Mora<\/li>\n<\/ul>\n<\/li>\n<li><strong>Tribunal<\/strong>\n<ul>\n<li>Presidente del tribunal: Francisco Palacios gambra <\/li>\n<li>Antonio Palenzuela lopez (vocal)<\/li>\n<li>marek Chauncey (vocal)<\/li>\n<li>mateo Alajarin ceron (vocal)<\/li>\n<\/ul>\n<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Tesis doctoral de Dorleta Otaegui Ansa En la presente tesis se estudia el dise\u00f1o y la s\u00edntesis qu\u00edmica de una [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","theme-transparent-header-meta":"","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center 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