N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads
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: | https://repositorio-aberto.up.pt/handle/10216/82063 |
Resumo: | The control of malaria is challenged by drug resistance, and new antimalarial drugs are needed. New drug discovery efforts include consideration of hybrid compounds as potential multitarget antimalarials. Previous work from our group has demonstrated that hybrid structures resulting from cinnamic acid conjugation with heterocyclic moieties from well-known antimalarials present improved antimalarial activity. Now, we report the synthesis and SAR analysis of an expanded series of cinnamic acid derivatives displaying remarkably high activities against both blood- and liver-stage malaria parasites. Two compounds judged most promising, based on their in vitro activity and druglikeness according to the Lipinski rules and Veber filter, were active in vivo against blood-stage rodent malaria parasites. Therefore, the compounds reported represent a new entry as promising dual-stage antimalarial leads. |
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N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial LeadsMedicina básicaBasic medicineThe control of malaria is challenged by drug resistance, and new antimalarial drugs are needed. New drug discovery efforts include consideration of hybrid compounds as potential multitarget antimalarials. Previous work from our group has demonstrated that hybrid structures resulting from cinnamic acid conjugation with heterocyclic moieties from well-known antimalarials present improved antimalarial activity. Now, we report the synthesis and SAR analysis of an expanded series of cinnamic acid derivatives displaying remarkably high activities against both blood- and liver-stage malaria parasites. Two compounds judged most promising, based on their in vitro activity and druglikeness according to the Lipinski rules and Veber filter, were active in vivo against blood-stage rodent malaria parasites. Therefore, the compounds reported represent a new entry as promising dual-stage antimalarial leads.20132013-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://repositorio-aberto.up.pt/handle/10216/82063eng0022-262310.1021/jm301654bBianca C PerezCatia TeixeiraInes S AlbuquerqueJiri GutPhilip J RosenthalJose R B GomesMiguel PrudencioPaula 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:RCAAP2023-11-29T15:12:56Zoai:repositorio-aberto.up.pt:10216/82063Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T00:18:10.466072Repositório 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 Chloroquine Analogues as Dual-Stage Antimalarial Leads |
title |
N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads |
spellingShingle |
N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads Bianca C Perez Medicina básica Basic medicine |
title_short |
N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads |
title_full |
N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads |
title_fullStr |
N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads |
title_full_unstemmed |
N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads |
title_sort |
N-Cinnamoylated Chloroquine Analogues as Dual-Stage Antimalarial Leads |
author |
Bianca C Perez |
author_facet |
Bianca C Perez Catia Teixeira Ines S Albuquerque Jiri Gut Philip J Rosenthal Jose R B Gomes Miguel Prudencio Paula Gomes |
author_role |
author |
author2 |
Catia Teixeira Ines S Albuquerque Jiri Gut Philip J Rosenthal Jose R B Gomes Miguel Prudencio Paula Gomes |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Bianca C Perez Catia Teixeira Ines S Albuquerque Jiri Gut Philip J Rosenthal Jose R B Gomes Miguel Prudencio Paula Gomes |
dc.subject.por.fl_str_mv |
Medicina básica Basic medicine |
topic |
Medicina básica Basic medicine |
description |
The control of malaria is challenged by drug resistance, and new antimalarial drugs are needed. New drug discovery efforts include consideration of hybrid compounds as potential multitarget antimalarials. Previous work from our group has demonstrated that hybrid structures resulting from cinnamic acid conjugation with heterocyclic moieties from well-known antimalarials present improved antimalarial activity. Now, we report the synthesis and SAR analysis of an expanded series of cinnamic acid derivatives displaying remarkably high activities against both blood- and liver-stage malaria parasites. Two compounds judged most promising, based on their in vitro activity and druglikeness according to the Lipinski rules and Veber filter, were active in vivo against blood-stage rodent malaria parasites. Therefore, the compounds reported represent a new entry as promising dual-stage antimalarial leads. |
publishDate |
2013 |
dc.date.none.fl_str_mv |
2013 2013-01-01T00:00:00Z |
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/10216/82063 |
url |
https://repositorio-aberto.up.pt/handle/10216/82063 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
0022-2623 10.1021/jm301654b |
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 |
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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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1799136100994777088 |