Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity

Detalhes bibliográficos
Autor(a) principal: Aguiar, Anna Caroline Campos
Data de Publicação: 2018
Outros Autores: Murce, Erika, Cortopassi, Wilian Augusto, Pimentel, Andre Silva, Almeida, Maria M. F. S., Barros, Daniele C. S., Guedes, Jéssica S., Meneghetti, Mauro Roberto, Krettli, Antoniana Ursine
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/33790
Resumo: 2020-01-01
id CRUZ_730b3476a66c0490b33395f153bb11bf
oai_identifier_str oai:www.arca.fiocruz.br:icict/33790
network_acronym_str CRUZ
network_name_str Repositório Institucional da FIOCRUZ (ARCA)
repository_id_str 2135
spelling Aguiar, Anna Caroline CamposMurce, ErikaCortopassi, Wilian AugustoPimentel, Andre SilvaAlmeida, Maria M. F. S.Barros, Daniele C. S.Guedes, Jéssica S.Meneghetti, Mauro RobertoKrettli, Antoniana Ursine2019-07-03T14:22:04Z2019-07-03T14:22:04Z2018AGUIAR, Anna Caroline Campos et al. Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity. International Journal for Parasitology: Drugs and Drug Resistance, v. 8, n. 3, p. 459-464, 2018.2211-3207https://www.arca.fiocruz.br/handle/icict/3379010.1016/j.ijpddr.2018.10.002engElsevierCloroquinaDesenho de drogasMalariaResistênciaChloroquineDrug designMalariaResistanceChloroquine analogs as antimalarial candidates with potent in vitro and in vivo activityinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article2020-01-01Fundação Oswaldo Cruz. Instituto Rene Rachou. Laboratório de Malária. Belo Horizonte, MG, Brasil.Pontifícia Universidade Católica do Rio de Janeiro. Departamento de Química. Rio de Janeiro, RJ, Brasil.Department of Pharmaceutical Chemistry. University of California. San Francisco, CA, USA.Pontifícia Universidade Católica do Rio de Janeiro. Departamento de Química. Rio de Janeiro, RJ, Brasil.Universidade Federal de Alagoas. Instituto de Química e Biotecnologia. Maceió, AL, Brasil.Universidade Federal de Alagoas. Instituto de Química e Biotecnologia. Maceió, AL, Brasil.Universidade Federal de Alagoas. Instituto de Química e Biotecnologia. Maceió, AL, Brasil.Universidade Federal de Alagoas. Instituto de Química e Biotecnologia. Maceió, AL, Brasil.Fundação Oswaldo Cruz. Instituto Rene Rachou. Laboratório de Malária. Belo Horizonte, MG, Brasil.In spite of recent efforts to eradicate malaria in the world, this parasitic disease is still considered a major public health problem, with a total of 216 million cases of malaria and 445,000 deaths in 2016. Artemisinin-based combination therapies remain effective in most parts of the world, but recent cases of resistance in Southeast Asia have urged for novel approaches to treat malaria caused by Plasmodium falciparum. In this work, we present chloroquine analogs that exhibited high activity against sensitive and chloroquine-resistant P. falciparum blood parasites and were also active against P. berghei infected mice. Among the compounds tested, DAQ, a chloroquine analog with a more linear side chain, was shown to be the most active in vitro and in vivo, with low cytotoxicity, and therefore may serve as the basis for the development of more effective chloroquine analogs to aid malaria eradication.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-83082https://www.arca.fiocruz.br/bitstream/icict/33790/1/license.txt9193a7c197bc67acd023525e72a03240MD51ORIGINALChloroquine analogs as antimalarial candidates.pdfChloroquine analogs as antimalarial candidates.pdfapplication/pdf3224012https://www.arca.fiocruz.br/bitstream/icict/33790/2/Chloroquine%20analogs%20as%20antimalarial%20candidates.pdfa7bd6de0491482c8fb605e9b310941e9MD52TEXTChloroquine analogs as antimalarial candidates.pdf.txtChloroquine analogs as antimalarial candidates.pdf.txtExtracted texttext/plain6https://www.arca.fiocruz.br/bitstream/icict/33790/3/Chloroquine%20analogs%20as%20antimalarial%20candidates.pdf.txt6d93d3216dc4a7f5df47d4876fbec4d3MD53icict/337902021-03-24 16:32:27.215oai:www.arca.fiocruz.br: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Repositório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352021-03-24T19:32:27Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
title Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
spellingShingle Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
Aguiar, Anna Caroline Campos
Cloroquina
Desenho de drogas
Malaria
Resistência
Chloroquine
Drug design
Malaria
Resistance
title_short Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
title_full Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
title_fullStr Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
title_full_unstemmed Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
title_sort Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
author Aguiar, Anna Caroline Campos
author_facet Aguiar, Anna Caroline Campos
Murce, Erika
Cortopassi, Wilian Augusto
Pimentel, Andre Silva
Almeida, Maria M. F. S.
Barros, Daniele C. S.
Guedes, Jéssica S.
Meneghetti, Mauro Roberto
Krettli, Antoniana Ursine
author_role author
author2 Murce, Erika
Cortopassi, Wilian Augusto
Pimentel, Andre Silva
Almeida, Maria M. F. S.
Barros, Daniele C. S.
Guedes, Jéssica S.
Meneghetti, Mauro Roberto
Krettli, Antoniana Ursine
author2_role author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Aguiar, Anna Caroline Campos
Murce, Erika
Cortopassi, Wilian Augusto
Pimentel, Andre Silva
Almeida, Maria M. F. S.
Barros, Daniele C. S.
Guedes, Jéssica S.
Meneghetti, Mauro Roberto
Krettli, Antoniana Ursine
dc.subject.other.pt_BR.fl_str_mv Cloroquina
Desenho de drogas
Malaria
Resistência
topic Cloroquina
Desenho de drogas
Malaria
Resistência
Chloroquine
Drug design
Malaria
Resistance
dc.subject.en.pt_BR.fl_str_mv Chloroquine
Drug design
Malaria
Resistance
description 2020-01-01
publishDate 2018
dc.date.issued.fl_str_mv 2018
dc.date.accessioned.fl_str_mv 2019-07-03T14:22:04Z
dc.date.available.fl_str_mv 2019-07-03T14:22:04Z
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.citation.fl_str_mv AGUIAR, Anna Caroline Campos et al. Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity. International Journal for Parasitology: Drugs and Drug Resistance, v. 8, n. 3, p. 459-464, 2018.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/33790
dc.identifier.issn.pt_BR.fl_str_mv 2211-3207
dc.identifier.doi.none.fl_str_mv 10.1016/j.ijpddr.2018.10.002
identifier_str_mv AGUIAR, Anna Caroline Campos et al. Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity. International Journal for Parasitology: Drugs and Drug Resistance, v. 8, n. 3, p. 459-464, 2018.
2211-3207
10.1016/j.ijpddr.2018.10.002
url https://www.arca.fiocruz.br/handle/icict/33790
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/33790/1/license.txt
https://www.arca.fiocruz.br/bitstream/icict/33790/2/Chloroquine%20analogs%20as%20antimalarial%20candidates.pdf
https://www.arca.fiocruz.br/bitstream/icict/33790/3/Chloroquine%20analogs%20as%20antimalarial%20candidates.pdf.txt
bitstream.checksum.fl_str_mv 9193a7c197bc67acd023525e72a03240
a7bd6de0491482c8fb605e9b310941e9
6d93d3216dc4a7f5df47d4876fbec4d3
bitstream.checksumAlgorithm.fl_str_mv MD5
MD5
MD5
repository.name.fl_str_mv Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)
repository.mail.fl_str_mv repositorio.arca@fiocruz.br
_version_ 1798325064974729216