S?ntese e avalia??o da atividade anticolinester?sica de novos derivados da piperina

• Author(s): Santos, Sabrina Neves
• Date: 2020
• Origin: Oasisbr
• Subject(s): Doen?a de Alzheimer; piperina; atividade anticolinester?sica; Alzheimer's disease; piperine; anticholinesterase activity; Qu?mica
• Document Type: Master thesis
• Language: Portuguese

Description

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Made available in DSpace on 2020-03-13T18:45:50Z (GMT). No. of bitstreams: 1 2013 - Sabrina Neves Santos.pdf: 4043550 bytes, checksum: 7c23cf3575011941dbe7a2492f6ee3f8 (MD5) Previous issue date: 2013-07-17

CAPES

The increase in life expectancy is a worldwide occurrence that shows the relative success of public health politics, But the increase in life expectancy has a negative effect: the appearance of degenerative diseases typical of old age, including several forms of dementia, like Alzheimer?s Disease (AD) that is certainly the most important. It is an irreversible and progressive disease characterized by neuronal deterioration. As a result this neuronal deterioration, the activity of cholinergic neurons that use the neurotransmitter acetylcholine (ACh) is reduced. One of the most promising approaches to treat this disease is to increase the level of acetylcholine in the brain using inhibitors of acetylcholinesterase (AChE). Therefore, this work aims to conduct structural modifications on the chemical structure of piperine and evaluate the influence of certain structural parameters, such as conformational flexibility and steric front of acetylcholinesterase activity (AChE and BChE) of these compounds, as well as make a kinetic study in order to discover what the profile of inhibition of AChE and BChE enzymes in order to find new compounds that could be useful in treating the symptoms of AD.

O aumento da expectativa de vida ? um fen?meno mundial que mostra o relativo sucesso de pol?ticas de sa?de p?blica, no entanto, o aumento da expectativa de vida tem como efeito negativo o aparecimento de doen?as degenerativas, t?picas de idades mais avan?adas, incluindo-se as v?rias formas de dem?ncia e entre estas, a mais importante ? a Doen?a de Alzheimer (DA), patologia irrevers?vel e progressiva caracterizada pela deteriora??o neuronal. Como resultado da neurodegenara??o, a atividade de neur?nios colin?rgicos, que utilizam o neurotransmissor acetilcolina (ACh), ? reduzida. Um dos mais promissores caminhos para tratar esta doen?a ? aumentar o n?vel de acetilcolina no c?rebro usando inibidores da acetilcolinesterase (AChE). Portanto, este trabalho tem como objetivo realizar modifica??es estruturais sobre a estrutura qu?mica da piperina e avaliar a influ?ncia de determinados par?metros estruturais, como a flexibilidade conformacional e o impedimento est?rico frente ? atividade anticolinester?sica (AChE e BChE) destes compostos, bem como fazer um estudo cin?tico a fim de descobrir qual o perfil de inibi??o das enzimas AChE e BChE, a fim de buscar novos compostos que poderiam ser ?teis no tratamento dos sintomas da DA.