Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/7322
Title: New approaches in antimalarial drug discovery and development - A Review
Authors: Aguiar, Anna Caroline Campos
Rocha, Eliana Maria Mauricio da
Souza, Nicolli Bellotti de
França, Tanos Celmar Costa
Krettli, Antoniana Ursine
Affilliation: Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brasil/ Universidade Federal de Minas Gerais. Programa de Pós-Graduação em Medicina Molecular. Belo Horizonte, MG, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brasil/ Universidade Federal de São João del Rey. Divinópolis, MG, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brasil/ Universidade Federal de Minas Gerais. Programa de Pós-Graduação em Medicina Molecular. Belo Horizonte, MG, Brasil
Abstract: Malaria remains a major world health problem following the emergence and spread of Plasmodium falciparum that is resistant to the majority of antimalarial drugs. This problem has since been aggravated by a decreased sensitivity of Plasmodium vivax to chloroquine. This review discusses strategies for evaluating the antimalarial activity of new compounds in vitro and in animal models ranging from conventional tests to the latest high-throughput screening technologies. Antimalarial discovery approaches include the following: the discovery of antimalarials from natural sources, chemical modifications of existing antimalarials, the development of hybrid compounds, test-ing of commercially available drugs that have been approved for human use for other diseases and molecular model-ling using virtual screening technology and docking. Using these approaches, thousands of new drugs with known molecular specificity and active against P. falciparum have been selected. The inhibition of haemozoin formation in vitro, an indirect test that does not require P. falciparum cultures, has been described and this test is believed to improve antimalarial drug discovery. Clinical trials conducted with new funds from international agencies and the participation of several industries committed to the eradication of malaria should accelerate the discovery of drugs that are as effective as artemisinin derivatives, thus providing new hope for the control of malaria.
Keywords: human malaria
Plasmodium falciparum
antimalarials
drug screening
chloroquine
artemisinin
drug resistance
Issue Date: 2012
Publisher: Fundação Oswaldo Cruz
Citation: AGUIAR, AnnCaroline Campos et al. New approaches in antimalarial drug discovery and development - A Review. Memórias do Instituto Oswaldo Cruz. 2012, vol.107, pp. 831-845.
DOI: 10.1590/S0074-02762012000700001
ISSN: 0074-0276
Copyright: open access
Appears in Collections:MG - IRR - Artigos de Periódicos

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