Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Repositório Institucional da UFLA |
Texto Completo: | http://repositorio.ufla.br/jspui/handle/1/48812 |
Resumo: | Pathologies related to disturbances of haemostasis and inflammation affect a large part of the world population. Among those illnesses, cardiovascular diseases such as cerebrovasculares diseases (CVD), ischemic heart disease, and cardiac failure are the main ones. Thus, the comprehension of the role and function of each biological structure in these mechanisms is fundamentally important, as well as the search for molecules able to modulate the components that act in these processes in an efficient and specific way, making the treatment and even healing of such diseases possible. Therefore, the research and synthesis of novel substances which show biological activities against inflammation and over haemostasis are of major importance. Chalcones and bis-chalcones are compounds that have shown a huge variety of pharmacological applications as anti-inflammatories, antioxidants, anticonvulsants, acetylcholinesterase inhibitors, antituberculosis, for cancer treatment, diabetes, etc. Furthermore, some characteristics of these molecules like simple synthesis pathways and high reaction yields make them targets of high interest for researchers all over the world. Additionally, the presence of hydrogens that can be replaced by several substituents provides an almost endless source of structures. In this work, four compounds were synthesized, which were 2 chalcone derivatives and 2 bis-chalcone derivatives. The synthesis were performed through Claisen-Schmidt condensation and the structures were characterized by Nuclear Magnetic Resonance (NMR). The biological properties of the molecules were evaluated by phospholipase, hemolytic, and clotting activities trials. The bis-chalcone derivative (1E,4E)- 1,5-bis(2-chlorophenyl)penta-1,4-dien-3-one showed good results retarding the clotting process and modulating the human phospholipid and erythrocyte degradation. Thus, this substance has the potential for application against cardiovascular diseases. However, more studies are needed to better understand its action mechanism. |
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Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasiaSynthesis of chalcones and bis-chalcones: study of protease modulators that act in hemostasis maintenanceModuladores enzimáticosCoagulação sanguíneaInflamaçãoSíntese orgânicaEnzyme modulatorsBlood clottingInflammationOrganic synthesisQuímicaPathologies related to disturbances of haemostasis and inflammation affect a large part of the world population. Among those illnesses, cardiovascular diseases such as cerebrovasculares diseases (CVD), ischemic heart disease, and cardiac failure are the main ones. Thus, the comprehension of the role and function of each biological structure in these mechanisms is fundamentally important, as well as the search for molecules able to modulate the components that act in these processes in an efficient and specific way, making the treatment and even healing of such diseases possible. Therefore, the research and synthesis of novel substances which show biological activities against inflammation and over haemostasis are of major importance. Chalcones and bis-chalcones are compounds that have shown a huge variety of pharmacological applications as anti-inflammatories, antioxidants, anticonvulsants, acetylcholinesterase inhibitors, antituberculosis, for cancer treatment, diabetes, etc. Furthermore, some characteristics of these molecules like simple synthesis pathways and high reaction yields make them targets of high interest for researchers all over the world. Additionally, the presence of hydrogens that can be replaced by several substituents provides an almost endless source of structures. In this work, four compounds were synthesized, which were 2 chalcone derivatives and 2 bis-chalcone derivatives. The synthesis were performed through Claisen-Schmidt condensation and the structures were characterized by Nuclear Magnetic Resonance (NMR). The biological properties of the molecules were evaluated by phospholipase, hemolytic, and clotting activities trials. The bis-chalcone derivative (1E,4E)- 1,5-bis(2-chlorophenyl)penta-1,4-dien-3-one showed good results retarding the clotting process and modulating the human phospholipid and erythrocyte degradation. Thus, this substance has the potential for application against cardiovascular diseases. However, more studies are needed to better understand its action mechanism.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)As patologias relacionadas a distúrbios da hemostasia e inflamação afligem grande parte da população mundial. Destacam-se, as doenças cardiovasculares como acidente vascular cerebral (AVC), doença isquêmica do coração e insuficiência cardíaca. Logo, compreender o papel e função de cada estrutura nestes mecanismos é de fundamental importância, bem como a busca por moléculas que possam modular de forma eficiente e específica componentes que atuam nestes processos, possibilitando o tratamento ou cura destas doenças. É, portanto, de suma importância a pesquisa e síntese de novas substâncias que apresentem atividade biológica no controle da inflamação e sob o mecanismo da hemostasia. As chalconas e bis- chalconas são substâncias que tem demonstrado grande variedade de aplicações farmacológicas como anti-inflamatória, antioxidante, anticonvulsivante, anti- acetilcolinesterase, antituberculose, para tratamento de câncer e diabetes, entre outras. Além disso, algumas características tornam essas moléculas alvos de grande interesse para pesquisadores ao redor do mundo, como por exemplo rotas de síntese relativamente simples, alto rendimento das reações, e a presença de hidrogênios que podem ser substituídos por uma enorme variedade de substituintes, o que possibilita, uma fonte praticamente inesgotável de estruturas. Nesse estudo foram sintetizados 4 compostos, sendo 2 derivados de chalconas e 2 de bis-chalconas, a síntese foi realizada por condensação de Claisen-Schimdt e caracterização das estruturas realizada por Ressonância Magnética Nuclear (RMN). O potencial biológico das moléculas foi avaliado em ensaios de atividade fosfolipásica, hemolítica e coagulante. O derivado de bis-chalcona, (1E,4E)-1,5-bis(2-clorofenil)penta-1,4-dien-3-ona apresentou bons resultados em retardar o processo de coagulação, e modular a degradação de fosfolipídios e eritrócitos humanos. Dessa forma, tal substância apresenta potencial para aplicação em doenças cardiovasculares, todavia é necessário mais testes e outros estudos para uma melhor compreensão de seu mecanismo de ação.Universidade Federal de LavrasPrograma de Pós-Graduação em AgroquímicaUFLAbrasilDepartamento de QuímicaMarcussi, SilvanaThomasi, Sérgio ScherrerMarcussi, SilvanaSouza, Josefina Aparecida deOliveira, Clayton ZambeliSilva, Matheus Henrique da Silva2022-01-12T15:51:04Z2022-01-12T15:51:04Z2021-01-122021-11-23info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfSILVA, M. H. da. Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia. 2021. 55 p. Dissertação (Mestrado em Agroquímica)-Universidade Federal de Lavras, Lavras, 2021.http://repositorio.ufla.br/jspui/handle/1/48812porinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFLAinstname:Universidade Federal de Lavras (UFLA)instacron:UFLA2022-01-12T15:51:04Zoai:localhost:1/48812Repositório InstitucionalPUBhttp://repositorio.ufla.br/oai/requestnivaldo@ufla.br || repositorio.biblioteca@ufla.bropendoar:2022-01-12T15:51:04Repositório Institucional da UFLA - Universidade Federal de Lavras (UFLA)false |
dc.title.none.fl_str_mv |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia Synthesis of chalcones and bis-chalcones: study of protease modulators that act in hemostasis maintenance |
title |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia |
spellingShingle |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia Silva, Matheus Henrique da Silva Moduladores enzimáticos Coagulação sanguínea Inflamação Síntese orgânica Enzyme modulators Blood clotting Inflammation Organic synthesis Química |
title_short |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia |
title_full |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia |
title_fullStr |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia |
title_full_unstemmed |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia |
title_sort |
Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia |
author |
Silva, Matheus Henrique da Silva |
author_facet |
Silva, Matheus Henrique da Silva |
author_role |
author |
dc.contributor.none.fl_str_mv |
Marcussi, Silvana Thomasi, Sérgio Scherrer Marcussi, Silvana Souza, Josefina Aparecida de Oliveira, Clayton Zambeli |
dc.contributor.author.fl_str_mv |
Silva, Matheus Henrique da Silva |
dc.subject.por.fl_str_mv |
Moduladores enzimáticos Coagulação sanguínea Inflamação Síntese orgânica Enzyme modulators Blood clotting Inflammation Organic synthesis Química |
topic |
Moduladores enzimáticos Coagulação sanguínea Inflamação Síntese orgânica Enzyme modulators Blood clotting Inflammation Organic synthesis Química |
description |
Pathologies related to disturbances of haemostasis and inflammation affect a large part of the world population. Among those illnesses, cardiovascular diseases such as cerebrovasculares diseases (CVD), ischemic heart disease, and cardiac failure are the main ones. Thus, the comprehension of the role and function of each biological structure in these mechanisms is fundamentally important, as well as the search for molecules able to modulate the components that act in these processes in an efficient and specific way, making the treatment and even healing of such diseases possible. Therefore, the research and synthesis of novel substances which show biological activities against inflammation and over haemostasis are of major importance. Chalcones and bis-chalcones are compounds that have shown a huge variety of pharmacological applications as anti-inflammatories, antioxidants, anticonvulsants, acetylcholinesterase inhibitors, antituberculosis, for cancer treatment, diabetes, etc. Furthermore, some characteristics of these molecules like simple synthesis pathways and high reaction yields make them targets of high interest for researchers all over the world. Additionally, the presence of hydrogens that can be replaced by several substituents provides an almost endless source of structures. In this work, four compounds were synthesized, which were 2 chalcone derivatives and 2 bis-chalcone derivatives. The synthesis were performed through Claisen-Schmidt condensation and the structures were characterized by Nuclear Magnetic Resonance (NMR). The biological properties of the molecules were evaluated by phospholipase, hemolytic, and clotting activities trials. The bis-chalcone derivative (1E,4E)- 1,5-bis(2-chlorophenyl)penta-1,4-dien-3-one showed good results retarding the clotting process and modulating the human phospholipid and erythrocyte degradation. Thus, this substance has the potential for application against cardiovascular diseases. However, more studies are needed to better understand its action mechanism. |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-01-12 2021-11-23 2022-01-12T15:51:04Z 2022-01-12T15:51:04Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/masterThesis |
format |
masterThesis |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
SILVA, M. H. da. Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia. 2021. 55 p. Dissertação (Mestrado em Agroquímica)-Universidade Federal de Lavras, Lavras, 2021. http://repositorio.ufla.br/jspui/handle/1/48812 |
identifier_str_mv |
SILVA, M. H. da. Síntese de chalconas e bis-chalconas: estudo de moduladores de proteases que atuam na manutenção da hemostasia. 2021. 55 p. Dissertação (Mestrado em Agroquímica)-Universidade Federal de Lavras, Lavras, 2021. |
url |
http://repositorio.ufla.br/jspui/handle/1/48812 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade Federal de Lavras Programa de Pós-Graduação em Agroquímica UFLA brasil Departamento de Química |
publisher.none.fl_str_mv |
Universidade Federal de Lavras Programa de Pós-Graduação em Agroquímica UFLA brasil Departamento de Química |
dc.source.none.fl_str_mv |
reponame:Repositório Institucional da UFLA instname:Universidade Federal de Lavras (UFLA) instacron:UFLA |
instname_str |
Universidade Federal de Lavras (UFLA) |
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UFLA |
institution |
UFLA |
reponame_str |
Repositório Institucional da UFLA |
collection |
Repositório Institucional da UFLA |
repository.name.fl_str_mv |
Repositório Institucional da UFLA - Universidade Federal de Lavras (UFLA) |
repository.mail.fl_str_mv |
nivaldo@ufla.br || repositorio.biblioteca@ufla.br |
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1807835106478391296 |