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Activity of bisnaphthalimidopropyl derivatives agains trypanosoma brucei.

Graça, Nuno A.G.; Gaspar, Luis; Costa, David M.; Loureiro, Inês; Thoo-Lin, Paul Kong; Ramos, Isbaal; Roura, Meritxell; Pruvost, Alain; Pemberton, Ian K.; Loukil, Hadjer; MacDougall, Jane; Tavares, Joana; Cordeiro-da-Silva, Anabela

Authors

Nuno A.G. Graça

Luis Gaspar

David M. Costa

Inês Loureiro

Paul Kong Thoo-Lin

Isbaal Ramos

Meritxell Roura

Alain Pruvost

Ian K. Pemberton

Hadjer Loukil

Jane MacDougall

Joana Tavares

Anabela Cordeiro-da-Silva



Abstract

Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or prone to elicit resistance. This study evaluated the activity of bisnaphthalimidopropyl (BNIP) derivatives against Trypanosoma brucei. BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showed in vitro inhibition in the single-unit nanomolar range, similar to the activity in the reference drug pentamidine, and presented low toxicity and adequate metabolic stability. Additionally, using a murine model of acute infection and live imaging, a significant decrease in parasite load in BNIPDabut-treated mice was observed. However, cure was not achieved. BNIPDabut constitutes a new scaffold for antitrypanosomal drugs that deserves further consideration.

Journal Article Type Article
Publication Date Apr 1, 2016
Journal Antimicrobial agents and chemotherapy
Print ISSN 0066-4804
Electronic ISSN 1098-6596
Publisher American Society for Microbiology
Peer Reviewed Peer Reviewed
Volume 60
Issue 4
Pages 2532-2536
Institution Citation GRACA, N.A.G., GASPAR, L, COSTA, D.M., LOUREIRO, I., KONG THOO-LING, P., RAMOS, I., ROURA, M., PRUVOST, A., PEMBERTON, I.K., LOUKIL, H., MACDOUGALL, J., TAVARES, J. and CORDEIRO-DA-SILVA, A. 2016. Activity of bisnaphthalimidopropyl derivatives agains trypanosoma brucei. Antimicrobial agents and chemotherapy [online], 60(4), pages 2532-2536. Available from: https://doi.org/10.1128/AAC.02490-15
DOI https://doi.org/10.1128/AAC.02490-15
Keywords BNIP; Trypanosoma brucei; Lead compounds; In vivo imaging; Drug screening

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