Activity of Bisnaphthalimidopropyl Derivatives against Trypanosoma brucei | Zendy

Nuno A. G. Graça | Zendy; Luís Gaspar | Zendy; David Costa | Zendy; Inês Loureiro | Zendy; Paul Kong Thoo Lin | Zendy; Isbaal Ramos | Zendy; Meritxell Roura | Zendy; Alain Pruvost | Zendy; Ian K. Pemberton | Zendy; Hadjer Loukil | Zendy; Jane MacDougall | Zendy; Joana Tavares | Zendy; Anabela CordeirodaSilva | Zendy

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Activity of Bisnaphthalimidopropyl Derivatives against Trypanosoma brucei

Author(s) -

Nuno A. G. Graça,

Luís Gaspar,

David Costa,

Inês Loureiro,

Paul Kong Thoo Lin,

Isbaal Ramos,

Meritxell Roura,

Alain Pruvost,

Ian K. Pemberton,

Hadjer Loukil,

Jane MacDougall,

Joana Tavares,

Anabela CordeirodaSilva

Publication year - 2016

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.02490-15

Subject(s) - trypanosoma brucei , biology , pharmacology , microbiology and biotechnology , biochemistry , gene

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 againstTrypanosoma brucei BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showedin vitroinhibition 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.

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