{"id":34464,"date":"1998-01-01T00:00:00","date_gmt":"1998-01-01T00:00:00","guid":{"rendered":"https:\/\/www.deberes.net\/tesis\/sin-categoria\/estudio-de-la-reactividad-de-4s-24-dimetil-24-dihidro-1h-pirazino21-b-quinazolina-36-diona-aplicado-a-la-sintesis-de-reversores-mdr\/"},"modified":"1998-01-01T00:00:00","modified_gmt":"1998-01-01T00:00:00","slug":"estudio-de-la-reactividad-de-4s-24-dimetil-24-dihidro-1h-pirazino21-b-quinazolina-36-diona-aplicado-a-la-sintesis-de-reversores-mdr","status":"publish","type":"post","link":"https:\/\/www.deberes.net\/tesis\/ciencias-medicas\/estudio-de-la-reactividad-de-4s-24-dimetil-24-dihidro-1h-pirazino21-b-quinazolina-36-diona-aplicado-a-la-sintesis-de-reversores-mdr\/","title":{"rendered":"Estudio de la reactividad de (4s)-2,4-dimetil-2,4-dihidro-1h-pirazino(2,1-b) quinazolina-3,6-diona aplicado a la sintesis de reversores mdr."},"content":{"rendered":"<h2>Tesis doctoral de <strong> Sonsoles Mart\u00edn Santamar\u00eda <\/strong><\/h2>\n<p>Se ha desarrollado una metodolog\u00eda general y con una elevada diastereoselecci\u00f3n para la s\u00edntesis de an\u00e1logos del reversor de mdr n-acetilardeemina, por alquilaci\u00f3n de la posici\u00f3n 1 del sistema (4s)-2,4-dimetil-1h-2, 4-dihidro-pirazino(2,1-b)quinazolina-3,6-diona (1). As\u00ed, ha sido posible la s\u00edntesis estereocontrolada de derivados 1-anti, 1-sin-monoalquilados y 1,1-dialquilados. Uno de ellos es unseco-an\u00e1logo de n-acetil-ardeemina. Se ha optimizado la dialquilaci\u00f3n de 1 debido al inter\u00e9s biol\u00f3gico de los derivados 1,1-disustituidos. Adem\u00e1s, se han obtenido derivados de 1 con la polaridad del c-1 invertida, y se ha demostrado que dicho sistema s\u00f3lo reacciona en condiciones de sn-1.  se han obtenido dos tipos diferentes de 11,11a-dihidroderivados de 1 para estudiar la influencia en la actividad biol\u00f3gica de la p\u00e9rdida de planaridad del anillo e. Los estudios de modelizaci\u00f3n realizados han avalado las conformaciones propuestas para los productos sintetizados. Los datos de actividad biol\u00f3gica muestran que los derivados 1-anti-monoalquilados no son activos, mientras que los 1-sin-monoalquilados tienen cierta actividad y los derivados 1,1-dialquilados son moderadamente activos.<\/p>\n<p>&nbsp;<\/p>\n<h3>Datos acad\u00e9micos de la tesis doctoral \u00ab<strong>Estudio de la reactividad de (4s)-2,4-dimetil-2,4-dihidro-1h-pirazino(2,1-b) quinazolina-3,6-diona aplicado a la sintesis de reversores mdr.<\/strong>\u00ab<\/h3>\n<ul>\n<li><strong>T\u00edtulo de la tesis:<\/strong>\u00a0 Estudio de la reactividad de (4s)-2,4-dimetil-2,4-dihidro-1h-pirazino(2,1-b) quinazolina-3,6-diona aplicado a la sintesis de reversores mdr. <\/li>\n<li><strong>Autor:<\/strong>\u00a0 Sonsoles Mart\u00edn Santamar\u00eda <\/li>\n<li><strong>Universidad:<\/strong>\u00a0 Complutense de Madrid<\/li>\n<li><strong>Fecha de lectura de la tesis:<\/strong>\u00a0 01\/01\/1998<\/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>Modesta Espada Lopez<\/li>\n<\/ul>\n<\/li>\n<li><strong>Tribunal<\/strong>\n<ul>\n<li>Presidente del tribunal: Jos\u00e9 Vicente Sinisterra Gago <\/li>\n<li>Albert Virgili Moya (vocal)<\/li>\n<li>Rosa Mar\u00eda Claramunt Vallesp\u00ed (vocal)<\/li>\n<li>Jos\u00e9 Luis Jim\u00e9nez Requejo (vocal)<\/li>\n<\/ul>\n<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Tesis doctoral de Sonsoles Mart\u00edn Santamar\u00eda Se ha desarrollado una metodolog\u00eda general y con una elevada diastereoselecci\u00f3n para la s\u00edntesis [&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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