Publication: Ligandos multidiana, una estrategia alternativa para el tratamiento de la enfermedad de Alzheimer
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2017-07-17
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Universidad Complutense de Madrid
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Abstract
La presente tesis doctoral titulada “LIGANDOS MULTIDIANA, UNA ESTRATEGIA ALTERNATIVA PARA EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER” se enmarca en un tema tan importante como es la investigación de terapias eficaces para luchar contra la enfermedad de Alzheimer. 1. INTRODUCCIÓN La enfermedad de Alzheimer (EA) es la causa más común de demencia, probablemente el 60-70% de todas las demencias, y una de las enfermedades con mayor repercusión en los países desarrollados. Estas enfermedades tienen un impacto dramático en la atención médica, así como implicaciones sociales y económicas debido a que los fármacos disponibles proporcionan un tratamiento sintomático temporal pero no detienen la progresión de la enfermedad. Desde 2003, cuando la FDA aprobó el uso clínico de la memantina, no se ha aprobado ningún otro fármaco para la EA. De hecho, todos los fármacos que se han evaluado en ensayos clínicos durante los últimos años han fracasado. Debido a la complejidad de la enfermedad, el descubrimiento de fármacos multidiana (MTDD) parece ser una buena opción para encontrar un tratamiento nuevo y eficaz para esta enfermedad. 2. OBJETIVO El objetivo fundamental del trabajo es desarrollar un fármaco capaz de actuar simultáneamente en dos o tres dianas terapéuticas involucradas en la EA, como son el receptor cannabinoide CB2, la enzima BACE-1 y la enzima BuChE. En este contexto, el objetivo de esta tesis ha sido el desarrollo de una nueva familia de derivados carbonílicos de 1-indazolilo que se comportan fármacos multidiana...
The present doctoral thesis entitled as “MULTITARGET LIGANDS, AN ALTERNATIVE STRATEGY FOR THE TREATMENT OF ALZHEIMER’S DISEASE” belongs to such an important area as the research into effective therapies to fight against the Alzheimer’s disease is. 1. INTRODUCTION Alzheimer’s disease (AD) is the most common cause of dementia, probably 60-70% of all dementias worldwide and one of the main causes of disease burden for developed regions. These diseases have a dramatic impact in medical care, as well as important social and economic implications, because the commercial drugs provide a temporary symptomatic treatment but do not stop the disease progression. Since 2003, when memantine was approved by FDA, it has not been approved any other drug to AD. In fact, all the drugs that are being studied in clinical trials in recent years have failed. Due to the complexity of the disease, the called multitarget drug discovery (MTDD), seems to be a good option to find a new and effective treatment against this disease. 2. OBJECTIVE The main objective of this project is to develop a drug able to act simultaneously in two or three therapeutic targets involved AD, such as the cannabinoid receptor CB2, BACE-1 and BuChE enzymes. Thus, in this context, the objective of this work has been the development of a new family of carbonyl derivatives of 1-indazolyl that it behaves as mutitarget drugs...
The present doctoral thesis entitled as “MULTITARGET LIGANDS, AN ALTERNATIVE STRATEGY FOR THE TREATMENT OF ALZHEIMER’S DISEASE” belongs to such an important area as the research into effective therapies to fight against the Alzheimer’s disease is. 1. INTRODUCTION Alzheimer’s disease (AD) is the most common cause of dementia, probably 60-70% of all dementias worldwide and one of the main causes of disease burden for developed regions. These diseases have a dramatic impact in medical care, as well as important social and economic implications, because the commercial drugs provide a temporary symptomatic treatment but do not stop the disease progression. Since 2003, when memantine was approved by FDA, it has not been approved any other drug to AD. In fact, all the drugs that are being studied in clinical trials in recent years have failed. Due to the complexity of the disease, the called multitarget drug discovery (MTDD), seems to be a good option to find a new and effective treatment against this disease. 2. OBJECTIVE The main objective of this project is to develop a drug able to act simultaneously in two or three therapeutic targets involved AD, such as the cannabinoid receptor CB2, BACE-1 and BuChE enzymes. Thus, in this context, the objective of this work has been the development of a new family of carbonyl derivatives of 1-indazolyl that it behaves as mutitarget drugs...
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Tesis inédita de la Universidad Complutense de Madrid, Facultad de Farmacia, Departamento de Química Orgánica y Farmacéutica, leída el 26/09/2016