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Synthetic Approaches and Computational Studies of Naturally Occurring Phenolic Carbohydrate Esters as Lead Pharmaceutics

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Resumo:Carbohydrates are vital for living systems and can contribute to the treatment of various diseases. However, more research is needed on sucrose-derived compounds due to their availability and low cost. Phenolic Sucrose Esters (PSEs), known for their antioxidant and anti-inflammatory properties, among others, are rarely synthesised, which, combined with the small amounts isolated from plants, limits their use in pharmacology. With this project, we explored one-step selective chemical methodologies, under Mitsunobu conditions, to synthesise a total of 14 biologically active sucrose esters: six mono- esters, which were our target compounds, resulting in a range of relatively good yields (17 – 33%), and additionally two per-acetylated mono-esters and six di-esters, all with promising applications. It is important to note that this is the first record of successfully synthesising 6,6’-di-O-feruloyl sucrose ester, 6,6’-di-O-sinapoyl sucrose ester, 6-O-syringyl sucrose ester, 6,6’-di-O-syringyl sucrose ester, 6-O-vanillyl sucrose ester, 6,6’-di-O-vanillyl sucrose ester and 1’,2,3,3’,4,4’,6’-hepta-O-acetil-6-O-benzoyl sucrose ester. A part of the project included a computational estimation of the radical scavenging effects of some of these compounds through different reaction pathways - hydrogen atom transfer (HAT), single electron transfer (SET) and radical adduct formation (RAF). Except for 6-O-benzoyl sucrose ester, all the mono-esters were able to deactivate the three free radicals used in the study (•ОСН3, •ООН, and •ООСН3) either in the HAT or in both HAT and RAF mechanisms.
Autores principais:Maciel, Verónica Raissa dos Santos
Assunto:sucrose phenolic sucrose esters esterification Mitsunobu reaction computational studies radical scavenging
Ano:2024
País:Portugal
Tipo de documento:dissertação de mestrado
Tipo de acesso:acesso aberto
Instituição associada:Universidade Nova de Lisboa
Idioma:inglês
Origem:Repositório Institucional da UNL
Descrição
Resumo:Carbohydrates are vital for living systems and can contribute to the treatment of various diseases. However, more research is needed on sucrose-derived compounds due to their availability and low cost. Phenolic Sucrose Esters (PSEs), known for their antioxidant and anti-inflammatory properties, among others, are rarely synthesised, which, combined with the small amounts isolated from plants, limits their use in pharmacology. With this project, we explored one-step selective chemical methodologies, under Mitsunobu conditions, to synthesise a total of 14 biologically active sucrose esters: six mono- esters, which were our target compounds, resulting in a range of relatively good yields (17 – 33%), and additionally two per-acetylated mono-esters and six di-esters, all with promising applications. It is important to note that this is the first record of successfully synthesising 6,6’-di-O-feruloyl sucrose ester, 6,6’-di-O-sinapoyl sucrose ester, 6-O-syringyl sucrose ester, 6,6’-di-O-syringyl sucrose ester, 6-O-vanillyl sucrose ester, 6,6’-di-O-vanillyl sucrose ester and 1’,2,3,3’,4,4’,6’-hepta-O-acetil-6-O-benzoyl sucrose ester. A part of the project included a computational estimation of the radical scavenging effects of some of these compounds through different reaction pathways - hydrogen atom transfer (HAT), single electron transfer (SET) and radical adduct formation (RAF). Except for 6-O-benzoyl sucrose ester, all the mono-esters were able to deactivate the three free radicals used in the study (•ОСН3, •ООН, and •ООСН3) either in the HAT or in both HAT and RAF mechanisms.