N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents
Autor(a) principal: | |
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Data de Publicação: | 2013 |
Outros Autores: | , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10773/19340 |
Resumo: | A series of cinnamic acid conjugates of primaquine and chloroquine were evaluated for their in vitro antileishmanial activities. Although primaquine derivatives had modest activity, chloroquine conjugates exhibited potent activity against both promastigotes (50% inhibitory concentration [IC50] = 2.6 to 21.8 mu M) and intramacrophagic amastigotes (IC50 = 1.2 to 9.3 mu M) of Leishmania infantum. Both the high activity of these chloroquine analogues and their mild-to-low toxicity toward host cells make them promising leads for the discovery of new antileishmanial agents. |
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N-Cinnamoylated Aminoquinolines as Promising Antileishmanial AgentsVISCERAL LEISHMANIASISDIAGNOSISDRUGSA series of cinnamic acid conjugates of primaquine and chloroquine were evaluated for their in vitro antileishmanial activities. Although primaquine derivatives had modest activity, chloroquine conjugates exhibited potent activity against both promastigotes (50% inhibitory concentration [IC50] = 2.6 to 21.8 mu M) and intramacrophagic amastigotes (IC50 = 1.2 to 9.3 mu M) of Leishmania infantum. Both the high activity of these chloroquine analogues and their mild-to-low toxicity toward host cells make them promising leads for the discovery of new antileishmanial agents.AMER SOC MICROBIOLOGY2017-12-07T19:09:23Z2013-01-01T00:00:00Z2013info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10773/19340eng0066-480410.1128/AAC.00557-13Vale-Costa, S.Costa-Gouveia, J.Perez, B.Silva, T.Teixeira, C.Gomes, P.Gomes, M. S.info: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:RCAAP2024-02-22T11:37:32Zoai:ria.ua.pt:10773/19340Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T02:54:08.280112Repositório 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 |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents |
title |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents |
spellingShingle |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents Vale-Costa, S. VISCERAL LEISHMANIASIS DIAGNOSIS DRUGS |
title_short |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents |
title_full |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents |
title_fullStr |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents |
title_full_unstemmed |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents |
title_sort |
N-Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents |
author |
Vale-Costa, S. |
author_facet |
Vale-Costa, S. Costa-Gouveia, J. Perez, B. Silva, T. Teixeira, C. Gomes, P. Gomes, M. S. |
author_role |
author |
author2 |
Costa-Gouveia, J. Perez, B. Silva, T. Teixeira, C. Gomes, P. Gomes, M. S. |
author2_role |
author author author author author author |
dc.contributor.author.fl_str_mv |
Vale-Costa, S. Costa-Gouveia, J. Perez, B. Silva, T. Teixeira, C. Gomes, P. Gomes, M. S. |
dc.subject.por.fl_str_mv |
VISCERAL LEISHMANIASIS DIAGNOSIS DRUGS |
topic |
VISCERAL LEISHMANIASIS DIAGNOSIS DRUGS |
description |
A series of cinnamic acid conjugates of primaquine and chloroquine were evaluated for their in vitro antileishmanial activities. Although primaquine derivatives had modest activity, chloroquine conjugates exhibited potent activity against both promastigotes (50% inhibitory concentration [IC50] = 2.6 to 21.8 mu M) and intramacrophagic amastigotes (IC50 = 1.2 to 9.3 mu M) of Leishmania infantum. Both the high activity of these chloroquine analogues and their mild-to-low toxicity toward host cells make them promising leads for the discovery of new antileishmanial agents. |
publishDate |
2013 |
dc.date.none.fl_str_mv |
2013-01-01T00:00:00Z 2013 2017-12-07T19:09:23Z |
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/10773/19340 |
url |
http://hdl.handle.net/10773/19340 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
0066-4804 10.1128/AAC.00557-13 |
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 |
AMER SOC MICROBIOLOGY |
publisher.none.fl_str_mv |
AMER SOC 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 |
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 |
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1799137593510592512 |