| Literature DB >> 26787703 |
Nuno A G Graça1, Luis Gaspar1, David M Costa1, Inês Loureiro1, Paul Kong Thoo-Lin2, Isbaal Ramos3, Meritxell Roura3, Alain Pruvost4, Ian K Pemberton5, Hadjer Loukil5, Jane MacDougall5, Joana Tavares6, Anabela Cordeiro-da-Silva7.
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.Entities:
Mesh：
Substances：
Year: 2016 PMID： 26787703 PMCID： PMC4808195 DOI： 10.1128/AAC.02490-15
Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191