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Activity of Bisnaphthalimidopropyl Derivatives against Trypanosoma brucei.

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 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.

SUBMITTER: Graca NA

PROVIDER: S-EPMC4808195 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature

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Activity of Bisnaphthalimidopropyl Derivatives against Trypanosoma brucei.

Graça Nuno A G NA Gaspar Luis L Costa David M DM Loureiro Inês I Thoo-Lin Paul Kong PK Ramos Isbaal I Roura Meritxell M Pruvost Alain A Pemberton Ian K IK Loukil Hadjer H MacDougall Jane J Tavares Joana J Cordeiro-da-Silva Anabela A

Antimicrobial agents and chemotherapy 20160325 4

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, usin ...[more]

PMID: 26787703

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