Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/33790
Title: Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
Authors: 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
Affilliation: Fundação 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.
Abstract: 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.
Keywords: Chloroquine
Drug design
Malaria
Resistance
keywords: Cloroquina
Desenho de drogas
Malaria
Resistência
Issue Date: 2018
Publisher: Elsevier
Citation: 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.
DOI: 10.1016/j.ijpddr.2018.10.002
ISSN: 2211-3207
Copyright: restricted access
Appears in Collections:MG - IRR - Artigos de Periódicos

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