Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei

Detalhes bibliográficos
Autor(a) principal: Loureiro, I
Data de Publicação: 2016
Outros Autores: Thoo-Lin, P, Ramos, I, Roura, M, Pruvost, A, Pemberton, I, Loukil, H, MacDougall, J, Tavares, J, Cordeiro-da-Silva, A, Graça, NA, Gaspar, L, Costa, DM
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: https://repositorio-aberto.up.pt/handle/10216/118203
Resumo: Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or prone to elicit resistance. This study evaluated the activity of bisnaphthalimidopropyl (BNIP) derivatives against Trypanosoma brucei. BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showed in vitro inhibition in the single-unit nanomolar range, similar to the activity in the reference drug pentamidine, and presented low toxicity and adequate metabolic stability. Additionally, using a murine model of acute infection and live imaging, a significant decrease in parasite load in BNIPDabut-treated mice was observed. However, cure was not achieved. BNIPDabut constitutes a new scaffold for antitrypanosomal drugs that deserves further consideration.
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spelling Activity of bisnaphthalimidopropyl derivatives against trypanosoma bruceiCurrent treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or prone to elicit resistance. This study evaluated the activity of bisnaphthalimidopropyl (BNIP) derivatives against Trypanosoma brucei. BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showed in vitro inhibition in the single-unit nanomolar range, similar to the activity in the reference drug pentamidine, and presented low toxicity and adequate metabolic stability. Additionally, using a murine model of acute infection and live imaging, a significant decrease in parasite load in BNIPDabut-treated mice was observed. However, cure was not achieved. BNIPDabut constitutes a new scaffold for antitrypanosomal drugs that deserves further consideration.American Society for Microbiology20162016-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://repositorio-aberto.up.pt/handle/10216/118203eng0066-480410.1128/AAC.02490-15Loureiro, IThoo-Lin, PRamos, IRoura, MPruvost, APemberton, ILoukil, HMacDougall, JTavares, JCordeiro-da-Silva, AGraça, NAGaspar, LCosta, DMinfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-11-29T14:06:30Zoai:repositorio-aberto.up.pt:10216/118203Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T23:54:57.054088Repositório 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 Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
title Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
spellingShingle Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
Loureiro, I
title_short Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
title_full Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
title_fullStr Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
title_full_unstemmed Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
title_sort Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
author Loureiro, I
author_facet Loureiro, I
Thoo-Lin, P
Ramos, I
Roura, M
Pruvost, A
Pemberton, I
Loukil, H
MacDougall, J
Tavares, J
Cordeiro-da-Silva, A
Graça, NA
Gaspar, L
Costa, DM
author_role author
author2 Thoo-Lin, P
Ramos, I
Roura, M
Pruvost, A
Pemberton, I
Loukil, H
MacDougall, J
Tavares, J
Cordeiro-da-Silva, A
Graça, NA
Gaspar, L
Costa, DM
author2_role author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Loureiro, I
Thoo-Lin, P
Ramos, I
Roura, M
Pruvost, A
Pemberton, I
Loukil, H
MacDougall, J
Tavares, J
Cordeiro-da-Silva, A
Graça, NA
Gaspar, L
Costa, DM
description Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or prone to elicit resistance. This study evaluated the activity of bisnaphthalimidopropyl (BNIP) derivatives against Trypanosoma brucei. BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showed in vitro inhibition in the single-unit nanomolar range, similar to the activity in the reference drug pentamidine, and presented low toxicity and adequate metabolic stability. Additionally, using a murine model of acute infection and live imaging, a significant decrease in parasite load in BNIPDabut-treated mice was observed. However, cure was not achieved. BNIPDabut constitutes a new scaffold for antitrypanosomal drugs that deserves further consideration.
publishDate 2016
dc.date.none.fl_str_mv 2016
2016-01-01T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://repositorio-aberto.up.pt/handle/10216/118203
url https://repositorio-aberto.up.pt/handle/10216/118203
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 0066-4804
10.1128/AAC.02490-15
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 American Society for Microbiology
publisher.none.fl_str_mv American Society for Microbiology
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
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
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collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
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