Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones

Detalhes bibliográficos
Autor(a) principal: Vale, Nuno
Data de Publicação: 2008
Outros Autores: Collins, Margaret S., Gut, Jiri, Ferraz, Ricardo, Rosenthal, Philip J., Cushion, Melanie T., Moreira, Rui, Gomes, Paula
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10400.22/20459
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 lg/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 lM range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead com pound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation.
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spelling Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-onesAIDSAntimalarialAntiplasmodialHIVInfectionMalariaPlasmodium falciparumPneumocystis cariniiPrimaqA 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 lg/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 lM range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead com pound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation.ElsevierRepositório Científico do Instituto Politécnico do PortoVale, NunoCollins, Margaret S.Gut, JiriFerraz, RicardoRosenthal, Philip J.Cushion, Melanie T.Moreira, RuiGomes, Paula2022-05-09T15:29:05Z2008-01-152008-01-15T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdftext/plain; charset=utf-8http://hdl.handle.net/10400.22/20459engVale, N., Collins, M. S., Gut, J., Ferraz, R., Rosenthal, P. J., Cushion, M. T., Moreira, R., & Gomes, P. (2008). Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones. Bioorganic & Medicinal Chemistry Letters, 18(2), 485-488. https://doi.org/https://doi.org/10.1016/j.bmcl.2007.11.1050960-894X10.1016/j.bmcl.2007.11.1051464-3405info: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:RCAAP2023-03-13T13:15:58Zoai:recipp.ipp.pt:10400.22/20459Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T17:40:31.913668Repositório 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
Vale, Nuno
AIDS
Antimalarial
Antiplasmodial
HIV
Infection
Malaria
Plasmodium falciparum
Pneumocystis carinii
Primaq
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 Vale, Nuno
author_facet Vale, Nuno
Collins, Margaret S.
Gut, Jiri
Ferraz, Ricardo
Rosenthal, Philip J.
Cushion, Melanie T.
Moreira, Rui
Gomes, Paula
author_role author
author2 Collins, Margaret S.
Gut, Jiri
Ferraz, Ricardo
Rosenthal, Philip J.
Cushion, Melanie T.
Moreira, Rui
Gomes, Paula
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório Científico do Instituto Politécnico do Porto
dc.contributor.author.fl_str_mv Vale, Nuno
Collins, Margaret S.
Gut, Jiri
Ferraz, Ricardo
Rosenthal, Philip J.
Cushion, Melanie T.
Moreira, Rui
Gomes, Paula
dc.subject.por.fl_str_mv AIDS
Antimalarial
Antiplasmodial
HIV
Infection
Malaria
Plasmodium falciparum
Pneumocystis carinii
Primaq
topic AIDS
Antimalarial
Antiplasmodial
HIV
Infection
Malaria
Plasmodium falciparum
Pneumocystis carinii
Primaq
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 lg/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 lM range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead com pound 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 2008-01-15
2008-01-15T00:00:00Z
2022-05-09T15:29:05Z
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 http://hdl.handle.net/10400.22/20459
url http://hdl.handle.net/10400.22/20459
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Vale, N., Collins, M. S., Gut, J., Ferraz, R., Rosenthal, P. J., Cushion, M. T., Moreira, R., & Gomes, P. (2008). Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones. Bioorganic & Medicinal Chemistry Letters, 18(2), 485-488. https://doi.org/https://doi.org/10.1016/j.bmcl.2007.11.105
0960-894X
10.1016/j.bmcl.2007.11.105
1464-3405
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
text/plain; charset=utf-8
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
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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