Exploring novel copper(II) binding azole compounds as potential antifungal drugs
Autor(a) principal: | |
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Data de Publicação: | 2022 |
Tipo de documento: | Dissertação |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10362/142192 |
Resumo: | "Invasive fungal infections are a major cause of morbidity and mortality among hospitalized patients and immunocompromised individuals. The increasing resistance of pathogenic fungi to the limited number of antifungal classes available makes the development of new and improved antifungals a pressing issue. This work aims to synthesize new azole compounds by molecular simplification of the model antifungal drug fluconazole while incorporating chemical functions that bind copper(II), to explore a potential synergy between the azoles and the metal. The target compounds designed are based on a central amine functionalized with three functions: an azole, a dihalogenobenzyl, and a varying copper(II) binding function. The 15 target compounds synthesized are organized in three families, which differ on the azole used (triazole or imidazole) and the length of the alkyl chain separating the central amine and the azole. Differences within each family are the copper(II) binding function used and, in one case, also the dihalogenobenzyl moiety. Such structural variations are expected to allow for a structure-activity relationship study based on the results of biological activity assays performed.(...)" |
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Exploring novel copper(II) binding azole compounds as potential antifungal drugsAntifungalazolecopperCandidaDomínio/Área Científica::Ciências Naturais"Invasive fungal infections are a major cause of morbidity and mortality among hospitalized patients and immunocompromised individuals. The increasing resistance of pathogenic fungi to the limited number of antifungal classes available makes the development of new and improved antifungals a pressing issue. This work aims to synthesize new azole compounds by molecular simplification of the model antifungal drug fluconazole while incorporating chemical functions that bind copper(II), to explore a potential synergy between the azoles and the metal. The target compounds designed are based on a central amine functionalized with three functions: an azole, a dihalogenobenzyl, and a varying copper(II) binding function. The 15 target compounds synthesized are organized in three families, which differ on the azole used (triazole or imidazole) and the length of the alkyl chain separating the central amine and the azole. Differences within each family are the copper(II) binding function used and, in one case, also the dihalogenobenzyl moiety. Such structural variations are expected to allow for a structure-activity relationship study based on the results of biological activity assays performed.(...)"Lima, LuísPimentel, CatarinaRUNPissarro, Teresa2022-04-062022-022025-04-30T00:00:00Z2022-04-06T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfhttp://hdl.handle.net/10362/142192TID:203210352enginfo:eu-repo/semantics/embargoedAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-03-11T05:19:41Zoai:run.unl.pt:10362/142192Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T03:50:11.851683Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs |
title |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs |
spellingShingle |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs Pissarro, Teresa Antifungal azole copper Candida Domínio/Área Científica::Ciências Naturais |
title_short |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs |
title_full |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs |
title_fullStr |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs |
title_full_unstemmed |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs |
title_sort |
Exploring novel copper(II) binding azole compounds as potential antifungal drugs |
author |
Pissarro, Teresa |
author_facet |
Pissarro, Teresa |
author_role |
author |
dc.contributor.none.fl_str_mv |
Lima, Luís Pimentel, Catarina RUN |
dc.contributor.author.fl_str_mv |
Pissarro, Teresa |
dc.subject.por.fl_str_mv |
Antifungal azole copper Candida Domínio/Área Científica::Ciências Naturais |
topic |
Antifungal azole copper Candida Domínio/Área Científica::Ciências Naturais |
description |
"Invasive fungal infections are a major cause of morbidity and mortality among hospitalized patients and immunocompromised individuals. The increasing resistance of pathogenic fungi to the limited number of antifungal classes available makes the development of new and improved antifungals a pressing issue. This work aims to synthesize new azole compounds by molecular simplification of the model antifungal drug fluconazole while incorporating chemical functions that bind copper(II), to explore a potential synergy between the azoles and the metal. The target compounds designed are based on a central amine functionalized with three functions: an azole, a dihalogenobenzyl, and a varying copper(II) binding function. The 15 target compounds synthesized are organized in three families, which differ on the azole used (triazole or imidazole) and the length of the alkyl chain separating the central amine and the azole. Differences within each family are the copper(II) binding function used and, in one case, also the dihalogenobenzyl moiety. Such structural variations are expected to allow for a structure-activity relationship study based on the results of biological activity assays performed.(...)" |
publishDate |
2022 |
dc.date.none.fl_str_mv |
2022-04-06 2022-02 2022-04-06T00:00:00Z 2025-04-30T00:00:00Z |
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 |
http://hdl.handle.net/10362/142192 TID:203210352 |
url |
http://hdl.handle.net/10362/142192 |
identifier_str_mv |
TID:203210352 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/embargoedAccess |
eu_rights_str_mv |
embargoedAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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1799138099275497472 |