Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil

Detalhes bibliográficos
Ano de defesa: 2013
Autor(a) principal: Simões, Maria Cecília Rodrigues lattes
Orientador(a): Viegas Júnior, Cláudio lattes
Banca de defesa: Dias, Danielle Ferreira, Viana, Gustavo Henrique Ribeiro
Tipo de documento: Dissertação
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Universidade Federal de Alfenas
Programa de Pós-Graduação: Programa de Pós-Graduação em Química
Departamento: Instituto de Química
País: Brasil
Palavras-chave em Português:
Doença de Alzheimer
Inibidores de Colinesterase
Fármacos do Sistema Nervoso Central
Área do conhecimento CNPq:
QUIMICA::QUIMICA ORGANICA
Link de acesso: https://repositorio.unifal-mg.edu.br/handle/123456789/377
Resumo: Alzheimer disease (AD) is a neurodegenerative disease clinically characterized by a progressive memory loss, which results in psychical and motor disfunction (FARRAN, JAMES, et al., 2011). Due to the large worldwide number of people with this disease, it is a challenge to science and public health. Therefore, projects aiming the disease symptomatic treatment and a patient progressive improvement are essential. Previous studies at the Laboratory of Phytochemistry and Medicinal Chemistry - LFQM -in Federal University of Alfenas - UNIFAL-MG, led to the discovery of the substance LFQM-18 (6 Figure 9) (new substance that presented a preliminary activity of acetylcholinesterase inhibitory), which was a prototype on the genesis of new compounds capable of acting as therapeutic agents in neurodegenerative diseases, especially Alzheimer's disease (AD). An analogous series of LFQM-18 was proposed and 10 new intermediary substances were synthesized and studied, validating the synthetic route for obtaining them. It was obtained, as a final product, acylhydrazone 17, evaluated preliminarily through Marston's test, which has indicated a low activity for the compound. Additional studies are ongoing to confirm the AChE inhibitory activity for compound 17.
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spelling Simões, Maria Cecília Rodrigueshttp://lattes.cnpq.br/1381066386437549Dias, Danielle FerreiraViana, Gustavo Henrique RibeiroViegas Júnior, Cláudiohttp://lattes.cnpq.br/85171953326079192015-06-12T22:44:37Z2013-02-01SIMÕES, Maria Cecília Rodrigues. Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil. 2013. 152 f. Dissertação (Mestrado em Química) - Universidade Federal de Alfenas, Alfenas, MG, 2013.https://repositorio.unifal-mg.edu.br/handle/123456789/377Alzheimer disease (AD) is a neurodegenerative disease clinically characterized by a progressive memory loss, which results in psychical and motor disfunction (FARRAN, JAMES, et al., 2011). Due to the large worldwide number of people with this disease, it is a challenge to science and public health. Therefore, projects aiming the disease symptomatic treatment and a patient progressive improvement are essential. Previous studies at the Laboratory of Phytochemistry and Medicinal Chemistry - LFQM -in Federal University of Alfenas - UNIFAL-MG, led to the discovery of the substance LFQM-18 (6 Figure 9) (new substance that presented a preliminary activity of acetylcholinesterase inhibitory), which was a prototype on the genesis of new compounds capable of acting as therapeutic agents in neurodegenerative diseases, especially Alzheimer's disease (AD). An analogous series of LFQM-18 was proposed and 10 new intermediary substances were synthesized and studied, validating the synthetic route for obtaining them. It was obtained, as a final product, acylhydrazone 17, evaluated preliminarily through Marston's test, which has indicated a low activity for the compound. Additional studies are ongoing to confirm the AChE inhibitory activity for compound 17.A Doença de Alzheimer (DA) é uma doença neurodegenerativa caracterizada clinicamente por uma perda progressiva de memória, que acarreta em disfunções psíquicas e motoras (FARRAN, JAMES, et al., 2011). Devido ao grande número de pessoas acometidas pela doença em todo o mundo, a mesma constitui um desafio a própria ciência e à saúde pública, e assim, projetos que visem o tratamento sintomático da doença e uma melhora progressiva do paciente são essenciais. Estudos anteriores no Laboratório de Fitoquímica e Química Medicinal – LFQM da Universidade Federal de Alfenas –UNIFAL-MG, levaram a descoberta da substância LFQM-18 (6 Figura 9) (substância inédita que apresentou uma atividade preliminar inibitória de acetilcolinesterase), que foi um protótipo na gênese de novos compostos capazes de atuar como agentes terapêuticos em doenças neurodegenerativas especialmente a Doença de Alzheimer (DA). Uma série análoga a LFQM-18 foi proposta e 10 novas substâncias intermediárias foram sintetizadas e estudadas, validando a rota sintética de obtenção das mesmas. Obteve-se como produto final a acilidrazona 17, avaliada preliminarmente através do teste de Marston, que indicou uma baixa atividade para o composto. Estudos adicionais estão em andamento para confirmar a atividade inibitória de AChE para o composto 17.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESapplication/pdfporUniversidade Federal de AlfenasPrograma de Pós-Graduação em QuímicaUNIFAL-MGBrasilInstituto de Químicainfo:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by-nc-nd/4.0/Doença de AlzheimerInibidores de ColinesteraseFármacos do Sistema Nervoso CentralQUIMICA::QUIMICA ORGANICAEstudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezilinfo:eu-repo/semantics/masterThesisinfo:eu-repo/semantics/publishedVersion1328253078826782306600600600-81940697172828021542075167498588264571reponame:Repositório Institucional da Universidade Federal de Alfenas - RiUnifalinstname:Universidade Federal de Alfenas (UNIFAL)instacron:UNIFALSimões, Maria Cecília RodriguesLICENSElicense.txtlicense.txttext/plain; charset=utf-81987https://repositorio.unifal-mg.edu.br/bitstreams/7915c3d5-777f-4f04-a00e-ba574359341f/download31555718c4fc75849dd08f27935d4f6bMD51CC-LICENSElicense_urllicense_urltext/plain; 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dc.title.pt-BR.fl_str_mv Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
title Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
spellingShingle Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
Simões, Maria Cecília Rodrigues
Doença de Alzheimer
Inibidores de Colinesterase
Fármacos do Sistema Nervoso Central
QUIMICA::QUIMICA ORGANICA
title_short Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
title_full Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
title_fullStr Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
title_full_unstemmed Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
title_sort Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil
author Simões, Maria Cecília Rodrigues
author_facet Simões, Maria Cecília Rodrigues
author_role author
dc.contributor.author.fl_str_mv Simões, Maria Cecília Rodrigues
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/1381066386437549
dc.contributor.referee1.fl_str_mv Dias, Danielle Ferreira
dc.contributor.referee2.fl_str_mv Viana, Gustavo Henrique Ribeiro
dc.contributor.advisor1.fl_str_mv Viegas Júnior, Cláudio
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/8517195332607919
contributor_str_mv Dias, Danielle Ferreira
Viana, Gustavo Henrique Ribeiro
Viegas Júnior, Cláudio
dc.subject.por.fl_str_mv Doença de Alzheimer
Inibidores de Colinesterase
Fármacos do Sistema Nervoso Central
topic Doença de Alzheimer
Inibidores de Colinesterase
Fármacos do Sistema Nervoso Central
QUIMICA::QUIMICA ORGANICA
dc.subject.cnpq.fl_str_mv QUIMICA::QUIMICA ORGANICA
description Alzheimer disease (AD) is a neurodegenerative disease clinically characterized by a progressive memory loss, which results in psychical and motor disfunction (FARRAN, JAMES, et al., 2011). Due to the large worldwide number of people with this disease, it is a challenge to science and public health. Therefore, projects aiming the disease symptomatic treatment and a patient progressive improvement are essential. Previous studies at the Laboratory of Phytochemistry and Medicinal Chemistry - LFQM -in Federal University of Alfenas - UNIFAL-MG, led to the discovery of the substance LFQM-18 (6 Figure 9) (new substance that presented a preliminary activity of acetylcholinesterase inhibitory), which was a prototype on the genesis of new compounds capable of acting as therapeutic agents in neurodegenerative diseases, especially Alzheimer's disease (AD). An analogous series of LFQM-18 was proposed and 10 new intermediary substances were synthesized and studied, validating the synthetic route for obtaining them. It was obtained, as a final product, acylhydrazone 17, evaluated preliminarily through Marston's test, which has indicated a low activity for the compound. Additional studies are ongoing to confirm the AChE inhibitory activity for compound 17.
publishDate 2013
dc.date.issued.fl_str_mv 2013-02-01
dc.date.accessioned.fl_str_mv 2015-06-12T22:44:37Z
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dc.identifier.citation.fl_str_mv SIMÕES, Maria Cecília Rodrigues. Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil. 2013. 152 f. Dissertação (Mestrado em Química) - Universidade Federal de Alfenas, Alfenas, MG, 2013.
dc.identifier.uri.fl_str_mv https://repositorio.unifal-mg.edu.br/handle/123456789/377
identifier_str_mv SIMÕES, Maria Cecília Rodrigues. Estudos visando a síntese e avaliação farmacológica de novos protótipos à fármacos inibidores de acetilcolinesterase planejados a partir do Donepezil. 2013. 152 f. Dissertação (Mestrado em Química) - Universidade Federal de Alfenas, Alfenas, MG, 2013.
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