Activity of bisnaphthalimidopropyl derivatives agains trypanosoma brucei.
Graca, Nuno A.G.
Costa, David M.
Kong Thoo Lin, Paul
Pemberton, Ian K.
MetadataShow full item record
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 agains trypanosoma brucei. Antimicrobial agents and chemotherapy [online], 60(4), pages 2532-2536. Available from: https://dx.doi.org/10.1128/AAC.02490-15
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.