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Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei.

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


Nuno A.G. Gra�a

Luis Gaspar

David M. Costa

In�s Loureiro

Isbaal Ramos

Meritxell Roura

Alain Pruvost

Ian K. Pemberton

Hadjer Loukil

Jane MacDougall

Joana Tavares

Anabela Cordeiro-da-Silva


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.


GRACA, N.A.G., GASPAR, L, COSTA, D.M., LOUREIRO, I., KONG THOO LIN, 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 against trypanosoma brucei. Antimicrobial agents and chemotherapy [online], 60(4), pages 2532-2536. Available from:

Journal Article Type Article
Acceptance Date Jan 15, 2016
Online Publication Date Mar 25, 2016
Publication Date Apr 1, 2016
Deposit Date Sep 13, 2016
Publicly Available Date Sep 26, 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
Keywords BNIP; Trypanosoma brucei; Lead compounds; In vivo imaging; Drug screening
Public URL


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