Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones
Autor(a) principal: | |
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Data de Publicação: | 2008 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | https://hdl.handle.net/10216/82118 |
Resumo: | A series of primaquine-derived imidazolidin-4-ones were screened for their in vitro activity against Pneumocystis carinii and Plasmodium falciparum W2 strain. Most compounds were active against P. carinii above 10 mu g/mL and displayed slight to marked activity. The imidazolidin-4-ones most active against P. carinii were also those most active antiplasmodial agents, in the mu M range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead compound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation. |
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Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-onesQuímicaChemical sciencesA series of primaquine-derived imidazolidin-4-ones were screened for their in vitro activity against Pneumocystis carinii and Plasmodium falciparum W2 strain. Most compounds were active against P. carinii above 10 mu g/mL and displayed slight to marked activity. The imidazolidin-4-ones most active against P. carinii were also those most active antiplasmodial agents, in the mu M range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead compound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation.20082008-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/10216/82118eng0960-894X10.1016/j.bmcl.2007.11.105Nuno ValeMargaret S CollinsJiri GutRicardo FerrazPhilip J RosenthalMelanie T CushioncRui MoreiraPaula Gomesinfo: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:RCAAP2023-11-29T15:09:09Zoai:repositorio-aberto.up.pt:10216/82118Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T00:16:53.199420Repositório 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 |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones |
title |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones |
spellingShingle |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones Nuno Vale Química Chemical sciences |
title_short |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones |
title_full |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones |
title_fullStr |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones |
title_full_unstemmed |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones |
title_sort |
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones |
author |
Nuno Vale |
author_facet |
Nuno Vale Margaret S Collins Jiri Gut Ricardo Ferraz Philip J Rosenthal Melanie T Cushionc Rui Moreira Paula Gomes |
author_role |
author |
author2 |
Margaret S Collins Jiri Gut Ricardo Ferraz Philip J Rosenthal Melanie T Cushionc Rui Moreira Paula Gomes |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Nuno Vale Margaret S Collins Jiri Gut Ricardo Ferraz Philip J Rosenthal Melanie T Cushionc Rui Moreira Paula Gomes |
dc.subject.por.fl_str_mv |
Química Chemical sciences |
topic |
Química Chemical sciences |
description |
A series of primaquine-derived imidazolidin-4-ones were screened for their in vitro activity against Pneumocystis carinii and Plasmodium falciparum W2 strain. Most compounds were active against P. carinii above 10 mu g/mL and displayed slight to marked activity. The imidazolidin-4-ones most active against P. carinii were also those most active antiplasmodial agents, in the mu M range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead compound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation. |
publishDate |
2008 |
dc.date.none.fl_str_mv |
2008 2008-01-01T00:00:00Z |
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://hdl.handle.net/10216/82118 |
url |
https://hdl.handle.net/10216/82118 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
0960-894X 10.1016/j.bmcl.2007.11.105 |
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.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 |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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 |
repository.mail.fl_str_mv |
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1799136089004310529 |