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Repositioning Salirasib as New Antimalarial Agent

preprint
submitted on 20.12.2018 and posted on 20.12.2018 by Exequiel O. J. Porta, Ignasi Bofill Verdaguer, Consuelo Perez, Claudia Banchio, Mauro Ferreira de Azevedo, Alejandro M Katzin, Guillermo Labadie

The antiplasmodial activity assay was performed using a simple, high-sensitivity methodology based on nanoluciferase (nLuc)-transfected P. falciparum parasites. The results showed that some of the analogs were active at low micromolar concentration. The most potent member of the series has S-farnesyl and the triazole moiety substituted with methyl-naphtyl. The low cytotoxicity in eukaryotic cells of the most active analogs provided good therapeutic indexes, being promising candidates for future antimalarial drugs development. Our results provide structure-activity relationship data for the design of new antimalarial drugs.

Funding

National Research Council of Argentina, CONICET (PIP 2009-11/0796 and 2012-14/0448)

Agencia Nacional de Promoción Científica y Tecnológica, ANPCyT- Argentina (PICT 2011/0589 to GRL)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP, 2017/22452-1)

History

Email Address of Submitting Author

labadie@iquir-conicet.gov.ar

Institution

IQUIR-CONICET

Country

Argentina

ORCID For Submitting Author

0000-0003-2467-1573

Declaration of Conflict of Interest

NO

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