Diseño, síntesis y evaluación biológica de nuevos compuestos antagonistas de los receptores y5 del neuropéptido y mchr-1 de la hormona concentradora de melanina como agentes para el tratamiento de la obesidad

• Autores: Laura Juanenea Irurueta
• Directores de la Tesis: Ignacio Aldana Moraza (dir. tes.), Antonio Monge Vega (codir. tes.)
• Lectura: En la Universidad de Navarra ( España ) en 2005
• Idioma: español
• Tribunal Calificador de la Tesis: Ofelia Nieto López (presid.), Silvia Perez Silanes (secret.), Salvador Vega Noverola (voc.), Ángel Berjón San Juan (voc.), Lara M. Orús Sarasola (voc.)
• Materias:
  • Química
    • Química orgánica
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• Resumen

  • TITULO: Diseño, síntesis y evaluación biológica DE nuevos compuestos antagonistas DE los receptores Y5 del neuropeptido y Y mchr-1 DE LA hormona concentradora DE melanina como agentes para EL tratamiento DE LA obesidad Resumen: obesity is now one of the most common and most important health problem in advanced and civilized societies because even mi Id obesity is conductive to many diseases, such as diabetes mellitus, arterial hypertension, dyslipidaemias, alimentary and respiratory disorders, and some types of cancer, all of which decrease life expectancy and the quality of life. Consequently, there is an urgent need for novel therapeutics that may help to stem the tide of the current epidemic. The regulation of appetite is a hiqhly integrated system involving numerous central and peripheral regulators, reflecting the complex nature of energy homeostasis. me hypothalamus is a key feeding center within the central nervous system (CNS), and many hypothalamic neuropeptides, such as NPY and melanin-concentrating hormone (MCH), play a pivotal role in the regulation of food intake and energy balance. Consequently, the aim of this study is the synthesis and biological evaluation of a series of novel compounds, which are structurally related to the arylsulfonamidomethylcyclohexyl moiety, in order to discover a novel compound that possesses antagonist activity on the NPY Y5 receptor, in the same way, we have begun to investigate the effects of new compounds as MCHR-1 receptor antagonists. We have identified a new series of (carbo)hydrazide derivative compounds as selective NPY Y5 receptor antagonists. We report the synthesis and structure activity relationships of these compounds and describe the identification of compounds with low nano-molar activity against the NPY Y5 receptor. As regards for MCHR-1 antagonists, we describe the first attempts to find a compound with antagonism against this receptor, in order to establish the structural charactenstics that must have the compounds blocking the MCHR-1, which is an important mediator of food intake