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Thiosalycilates v04-ChemRxiv.pdf (916.25 kB)

Repositioning Salirasib as New Antimalarial Agent

preprint
submitted on 20.12.2018, 11:31 and posted on 20.12.2018, 16:50 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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